Home MAPK Raf inhibitor Sorafenib (BAY 43-9006)

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Sorafenib (BAY 43-9006) Raf/VEGFR inhibitor

제품 번호: S7397

Sorafenib is a multikinase inhibitor of Raf-1 and B-Raf with IC50 of 6 nM and 22 nM in cell-free assays, respectively. Sorafenib inhibits VEGFR-2, VEGFR-3, PDGFR-β, Flt-3 and c-KIT with IC50 of 90 nM, 20 nM, 57 nM, 59 nM and 68 nM, respectively. Sorafenib induces autophagy and apoptosis and activates ferroptosis with anti-tumor activity.
Sorafenib (BAY 43-9006) Raf inhibitor Chemical Structure

화학 구조

분자량: 464.82

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품질 관리 (Quality Control)

배치: 순도: 99.91%
99.91

세포 배양, 처리 및 작업 농도
(Cell Culture, Treatment & Working Concentration)

세포주 분석 유형 농도 배양 시간 제형 활성 설명 PMID
MV-4-11 Growth Inhibition Assay IC50=0.00000303 μM SANGER
MONO-MAC-6 Growth Inhibition Assay IC50=0.00418 μM SANGER
ALL-PO Growth Inhibition Assay IC50=0.03184 μM SANGER
NKM-1 Growth Inhibition Assay IC50=0.07416 μM SANGER
CGTH-W-1 Growth Inhibition Assay IC50=0.25022 μM SANGER
BB65-RCC Growth Inhibition Assay IC50=0.47073 μM SANGER
NOS-1 Growth Inhibition Assay IC50=0.5636 μM SANGER
SH-4 Growth Inhibition Assay IC50=0.65613 μM SANGER
HOP-62 Growth Inhibition Assay IC50=0.85088 μM SANGER
HCC2998 Growth Inhibition Assay IC50=0.88818 μM SANGER
GDM-1 Growth Inhibition Assay IC50=0.90698 μM SANGER
KM12 Growth Inhibition Assay IC50=1.02098 μM SANGER
LB2518-MEL Growth Inhibition Assay IC50=1.20809 μM SANGER
NCI-H1436 Growth Inhibition Assay IC50=1.21678 μM SANGER
EM-2 Growth Inhibition Assay IC50=1.35578 μM SANGER
LAMA-84 Growth Inhibition Assay IC50=1.37648 μM SANGER
KG-1 Growth Inhibition Assay IC50=1.47935 μM SANGER
A388 Growth Inhibition Assay IC50=1.59165 μM SANGER
no-10 Growth Inhibition Assay IC50=1.61726 μM SANGER
SF126 Growth Inhibition Assay IC50=1.63812 μM SANGER
MEG-01 Growth Inhibition Assay IC50=1.8098 μM SANGER
A3-KAW Growth Inhibition Assay IC50=1.8842 μM SANGER
D-247MG Growth Inhibition Assay IC50=2.1448 μM SANGER
OVCAR-4 Growth Inhibition Assay IC50=2.21393 μM SANGER
NCI-SNU-1 Growth Inhibition Assay IC50=2.3162 μM SANGER
NCI-H2171 Growth Inhibition Assay IC50=2.39764 μM SANGER
SIG-M5 Growth Inhibition Assay IC50=2.42242 μM SANGER
BE-13 Growth Inhibition Assay IC50=2.69609 μM SANGER
K052 Growth Inhibition Assay IC50=2.74616 μM SANGER
L-540 Growth Inhibition Assay IC50=2.75789 μM SANGER
KMOE-2 Growth Inhibition Assay IC50=2.8135 μM SANGER
MFH-ino Growth Inhibition Assay IC50=2.92185 μM SANGER
HL-60 Growth Inhibition Assay IC50=3.06299 μM SANGER
HCC2218 Growth Inhibition Assay IC50=3.12003 μM SANGER
TE-5 Growth Inhibition Assay IC50=3.13162 μM SANGER
MZ1-PC Growth Inhibition Assay IC50=3.47509 μM SANGER
MRK-nu-1 Growth Inhibition Assay IC50=3.61468 μM SANGER
MZ7-mel Growth Inhibition Assay IC50=3.66099 μM SANGER
BC-1 Growth Inhibition Assay IC50=3.7402 μM SANGER
ST486 Growth Inhibition Assay IC50=3.83673 μM SANGER
KS-1 Growth Inhibition Assay IC50=3.88198 μM SANGER
SK-NEP-1 Growth Inhibition Assay IC50=4.16815 μM SANGER
BC-3 Growth Inhibition Assay IC50=4.23391 μM SANGER
NCI-H1581 Growth Inhibition Assay IC50=4.28798 μM SANGER
MHH-PREB-1 Growth Inhibition Assay IC50=4.40484 μM SANGER
NOMO-1 Growth Inhibition Assay IC50=4.48905 μM SANGER
QIMR-WIL Growth Inhibition Assay IC50=5.07294 μM SANGER
SF539 Growth Inhibition Assay IC50=5.13227 μM SANGER
TE-12 Growth Inhibition Assay IC50=5.24929 μM SANGER
NCI-H510A Growth Inhibition Assay IC50=5.41685 μM SANGER
JAR Growth Inhibition Assay IC50=5.50824 μM SANGER
no-11 Growth Inhibition Assay IC50=5.73568 μM SANGER
BV-173 Growth Inhibition Assay IC50=5.95682 μM SANGER
SR Growth Inhibition Assay IC50=6.00678 μM SANGER
MOLT-16 Growth Inhibition Assay IC50=6.25266 μM SANGER
MZ2-MEL Growth Inhibition Assay IC50=6.31839 μM SANGER
SW954 Growth Inhibition Assay IC50=6.45866 μM SANGER
ML-2 Growth Inhibition Assay IC50=6.52849 μM SANGER
OCI-AML2 Growth Inhibition Assay IC50=6.61062 μM SANGER
SIMA Growth Inhibition Assay IC50=7.00101 μM SANGER
DOHH-2 Growth Inhibition Assay IC50=7.05676 μM SANGER
697 Growth Inhibition Assay IC50=7.05989 μM SANGER
NB1 Growth Inhibition Assay IC50=7.40407 μM SANGER
D-392MG Growth Inhibition Assay IC50=7.62663 μM SANGER
ES8 Growth Inhibition Assay IC50=7.76503 μM SANGER
RPMI-8226 Growth Inhibition Assay IC50=7.84511 μM SANGER
IST-MEL1 Growth Inhibition Assay IC50=8.40002 μM SANGER
NB14 Growth Inhibition Assay IC50=8.63133 μM SANGER
HD-MY-Z Growth Inhibition Assay IC50=8.63746 μM SANGER
TE-10 Growth Inhibition Assay IC50=8.76353 μM SANGER
LC-1F Growth Inhibition Assay IC50=9.10834 μM SANGER
OS-RC-2 Growth Inhibition Assay IC50=9.11243 μM SANGER
NCI-SNU-16 Growth Inhibition Assay IC50=9.21026 μM SANGER
SHP-77 Growth Inhibition Assay IC50=9.71662 μM SANGER
A4-Fuk Growth Inhibition Assay IC50=9.7561 μM SANGER
NB6 Growth Inhibition Assay IC50=9.76029 μM SANGER
JiyoyeP-2003 Growth Inhibition Assay IC50=10.4745 μM SANGER
DMS-114 Growth Inhibition Assay IC50=10.5441 μM SANGER
NB7 Growth Inhibition Assay IC50=10.7526 μM SANGER
NCI-H747 Growth Inhibition Assay IC50=11.1216 μM SANGER
HH Growth Inhibition Assay IC50=11.3876 μM SANGER
EW-18 Growth Inhibition Assay IC50=11.9044 μM SANGER
CHP-126 Growth Inhibition Assay IC50=11.9738 μM SANGER
NTERA-S-cl-D1 Growth Inhibition Assay IC50=12.0278 μM SANGER
DEL Growth Inhibition Assay IC50=12.0985 μM SANGER
LU-139 Growth Inhibition Assay IC50=12.5413 μM SANGER
P30-OHK Growth Inhibition Assay IC50=12.5479 μM SANGER
NCI-H1522 Growth Inhibition Assay IC50=12.746 μM SANGER
NCI-H1299 Growth Inhibition Assay IC50=13.2911 μM SANGER
UACC-257 Growth Inhibition Assay IC50=13.5126 μM SANGER
Calu-6 Growth Inhibition Assay IC50=13.6046 μM SANGER
NCI-H1882 Growth Inhibition Assay IC50=13.8555 μM SANGER
BB30-HNC Growth Inhibition Assay IC50=14.0609 μM SANGER
ES1 Growth Inhibition Assay IC50=14.1551 μM SANGER
NCI-H1694 Growth Inhibition Assay IC50=14.4811 μM SANGER
IST-SL1 Growth Inhibition Assay IC50=14.9616 μM SANGER
ECC4 Growth Inhibition Assay IC50=15.0558 μM SANGER
MDA-MB-134-VI Growth Inhibition Assay IC50=15.4131 μM SANGER
SCH Growth Inhibition Assay IC50=15.4728 μM SANGER
SK-N-FI Growth Inhibition Assay IC50=15.6534 μM SANGER
HDLM-2 Growth Inhibition Assay IC50=16.0714 μM SANGER
Ramos-2G6-4C10 Growth Inhibition Assay IC50=16.1297 μM SANGER
EW-24 Growth Inhibition Assay IC50=16.1661 μM SANGER
NCI-H2141 Growth Inhibition Assay IC50=16.189 μM SANGER
LC4-1 Growth Inhibition Assay IC50=16.6119 μM SANGER
HT-144 Growth Inhibition Assay IC50=17.006 μM SANGER
SK-MEL-1 Growth Inhibition Assay IC50=17.0072 μM SANGER
SCC-15 Growth Inhibition Assay IC50=17.1638 μM SANGER
C8166 Growth Inhibition Assay IC50=17.6833 μM SANGER
GOTO Growth Inhibition Assay IC50=17.8344 μM SANGER
COR-L279 Growth Inhibition Assay IC50=18.1362 μM SANGER
K-562 Growth Inhibition Assay IC50=18.7143 μM SANGER
ES3 Growth Inhibition Assay IC50=18.8041 μM SANGER
LU-165 Growth Inhibition Assay IC50=19.7008 μM SANGER
KM-H2 Growth Inhibition Assay IC50=20.3184 μM SANGER
RL Growth Inhibition Assay IC50=20.9692 μM SANGER
EW-3 Growth Inhibition Assay IC50=21.1889 μM SANGER
A101D Growth Inhibition Assay IC50=21.3752 μM SANGER
HUTU-80 Growth Inhibition Assay IC50=21.3946 μM SANGER
NCI-H23 Growth Inhibition Assay IC50=21.3992 μM SANGER
PF-382 Growth Inhibition Assay IC50=21.4403 μM SANGER
LB373-MEL-D Growth Inhibition Assay IC50=21.5615 μM SANGER
TE-8 Growth Inhibition Assay IC50=21.6394 μM SANGER
TE-9 Growth Inhibition Assay IC50=21.8513 μM SANGER
Daudi Growth Inhibition Assay IC50=21.9304 μM SANGER
D-542MG Growth Inhibition Assay IC50=22.0256 μM SANGER
U-698-M Growth Inhibition Assay IC50=22.4603 μM SANGER
ES6 Growth Inhibition Assay IC50=22.7366 μM SANGER
DU-4475 Growth Inhibition Assay IC50=23.8897 μM SANGER
ECC12 Growth Inhibition Assay IC50=24.2803 μM SANGER
C2BBe1 Growth Inhibition Assay IC50=24.3239 μM SANGER
IST-SL2 Growth Inhibition Assay IC50=24.4362 μM SANGER
DJM-1 Growth Inhibition Assay IC50=24.5221 μM SANGER
DMS-153 Growth Inhibition Assay IC50=24.8614 μM SANGER
NB13 Growth Inhibition Assay IC50=25.0265 μM SANGER
SK-N-DZ Growth Inhibition Assay IC50=26.3414 μM SANGER
COR-L88 Growth Inhibition Assay IC50=26.5796 μM SANGER
LU-65 Growth Inhibition Assay IC50=26.8535 μM SANGER
TGBC1TKB Growth Inhibition Assay IC50=26.9828 μM SANGER
THP-1 Growth Inhibition Assay IC50=27.2141 μM SANGER
ONS-76 Growth Inhibition Assay IC50=27.332 μM SANGER
LC-2-ad Growth Inhibition Assay IC50=27.6231 μM SANGER
EW-13 Growth Inhibition Assay IC50=29.1746 μM SANGER
MS-1 Growth Inhibition Assay IC50=30.7278 μM SANGER
NCI-H2227 Growth Inhibition Assay IC50=30.9806 μM SANGER
LXF-289 Growth Inhibition Assay IC50=31.4492 μM SANGER
MC116 Growth Inhibition Assay IC50=32.0826 μM SANGER
EVSA-T Growth Inhibition Assay IC50=32.2585 μM SANGER
CTB-1 Growth Inhibition Assay IC50=33.1101 μM SANGER
COLO-320-HSR Growth Inhibition Assay IC50=33.1603 μM SANGER
NCI-H2196 Growth Inhibition Assay IC50=33.2557 μM SANGER
LB2241-RCC Growth Inhibition Assay IC50=33.3135 μM SANGER
LS-513 Growth Inhibition Assay IC50=33.8638 μM SANGER
LP-1 Growth Inhibition Assay IC50=33.9956 μM SANGER
A253 Growth Inhibition Assay IC50=34.2296 μM SANGER
SK-MM-2 Growth Inhibition Assay IC50=34.9451 μM SANGER
NCI-H1963 Growth Inhibition Assay IC50=35.3072 μM SANGER
MMAC-SF Growth Inhibition Assay IC50=35.8785 μM SANGER
LB831-BLC Growth Inhibition Assay IC50=36.0654 μM SANGER
WSU-NHL Growth Inhibition Assay IC50=36.164 μM SANGER
CESS Growth Inhibition Assay IC50=36.2848 μM SANGER
NEC8 Growth Inhibition Assay IC50=36.5835 μM SANGER
KNS-42 Growth Inhibition Assay IC50=37.1237 μM SANGER
MHH-CALL-2 Growth Inhibition Assay IC50=37.1821 μM SANGER
K5 Growth Inhibition Assay IC50=38.43 μM SANGER
CP66-MEL Growth Inhibition Assay IC50=39.0733 μM SANGER
OPM-2 Growth Inhibition Assay IC50=39.8432 μM SANGER
IST-MES1 Growth Inhibition Assay IC50=40.3096 μM SANGER
EC-GI-10 Growth Inhibition Assay IC50=41.5805 μM SANGER
CTV-1 Growth Inhibition Assay IC50=42.8406 μM SANGER
DG-75 Growth Inhibition Assay IC50=43.7595 μM SANGER
KNS-81-FD Growth Inhibition Assay IC50=45.4058 μM SANGER
NCI-H82 Growth Inhibition Assay IC50=45.5758 μM SANGER
RPMI-8866 Growth Inhibition Assay IC50=46.1873 μM SANGER
ACN Growth Inhibition Assay IC50=46.434 μM SANGER
NCI-H1395 Growth Inhibition Assay IC50=46.4756 μM SANGER
NCI-H209 Growth Inhibition Assay IC50=47.1405 μM SANGER
TGW Growth Inhibition Assay IC50=49.0791 μM SANGER
NCI-H748 Growth Inhibition Assay IC50=49.4753 μM SANGER
EKVX Growth Inhibition Assay IC50=49.6628 μM SANGER
MV4-11 Antiproliferative activity assay IC50 = 0.00087 μM 19754199
MV4-11 Cytotoxicity assay IC50 = 0.00087 μM 19654408
TT Antiproliferative activity assay IC50 = 0.0014 μM 18849971
RS4-11 Function assay IC50 = 0.002 μM 19654408
MOLM13 Function assay IC50 = 0.002 μM 24641103
Sf9 Function assay IC50 = 0.003 μM 21708468
RS4-11 Function assay IC50 = 0.0032 μM 19654408
MV4-11 Growth inhibition assay IC50 = 0.004 μM 29357250
A375 Function assay IC50 = 0.0044 μM 29461827
MOLM13 Antiproliferative activity assay IC50 = 0.005 μM 24641103
MV4-11 Function assay IC50 = 0.007 μM 23362959
MV4-11 Cytotoxicity assay IC50 = 0.007 μM 26342867
HEK293 Function assay Kd = 0.013 μM 19754199
Kasumi-1 Antiproliferative activity assay IC50 = 0.015 μM 20570526
MV4-11 Antiproliferative activity assay IC50 = 0.015 μM 20570526
sf9 Function assay IC50 = 0.015 μM 29266937
sf9 Function assay IC50 = 0.018 μM 21708468
sf9 Function assay IC50 = 0.02 μM 23618709
MV4-11 Antiproliferative activity assay GI50 = 0.03 μM 21708468
Sf9 Function assay IC50 = 0.042 μM 26081023
SF9 Function assay IC50 = 0.043 μM 18473434
MV4-11 Cytotoxicity assay GI50 = 0.043 μM 23618709
MV4-11 Function assay GI50 = 0.043 μM 26081023
SF9 Function assay IC50 = 0.044 μM 26081023
SF9 Function assay IC50 = 0.054 μM 21708468
SF9 Function assay IC50 = 0.054 μM 23618709
MOLM13 Antiproliferative activity assay GI50 = 0.056 μM 21708468
MOLM13 Antiproliferative activity assay GI50 = 0.056 μM 22726931
MOLM13 Cytotoxicity assay GI50 = 0.056 μM 23618709
MOLM-13 Function assay GI50 = 0.056 μM 26081023
SF9 Function assay IC50 = 0.058 μM 29266937
WM266.4 Antiproliferative activity assay IC50 = 0.06 μM 25496804
MDA-MB-231 Function assay IC50 = 0.063 μM 28431342
SF9 Function assay IC50 = 0.09 μM 29266937
Spodoptera frugiperda Function assay IC50 = 0.09 μM 26922228
SF9 Function assay IC50 = 0.09 μM 23562241
SF9 Function assay IC50 = 0.1 μM 23442188
SF9 Function assay IC50 = 0.1 μM 23442188
HEK293 Function assay IC50 = 0.12 μM 26318998
MCF7 Antiproliferative activity assay IC50 = 0.19 μM 25496804
MV4-11 Antiproliferative activity human IC50 = 0.3 μM 28242553
HepG2 Antiproliferative activity assay EC50 = 0.302 μM 27010810
THP1 Antiproliferative activity assay IC50 = 0.31 μM 20570526
SMMC7721 Cytotoxicity assay IC50 = 0.37 μM 25982075
HT-29 Antiproliferative activity assay IC50 = 0.39 μM 25778995
sf9 Function assay Kd = 0.6 μM 28109791
T47D Antiproliferative activity assay IC50 = 0.61 μM 25778995
A549 Cytotoxicity assay IC50 = 0.63 μM 25982075
HeLa Cytotoxicity assay IC50 = 0.64 μM 30015070
WM3629 Antiproliferative activity assay GI50 = 0.65 μM 20466542
SMMC7721 Antiproliferative activity assay IC50 = 0.65 μM 26342134
WM3629 Growth inhibition assay GI50 = 0.78 μM 20149658
WM3629 Antiproliferative activity assay GI50 = 0.78 μM 26810260
MCF7 Antiproliferative activity assay IC50 = 0.78 μM 25778995
K562 Antiproliferative activity assay IC50 = 0.86 μM 24315192
COLO205 Antiproliferative activity assay IC50 = 0.87 μM 25778995
T29 Cytotoxicity assay IC50 = 0.9 μM 26318998
MDA-MB-231 Cytotoxicity assay IC50 = 0.94 μM 25086238
MDA-MB-231 Cytotoxicity assay IC50 = 0.94 μM 25440879
HepG2 Antiproliferative activity assay IC50 = 1.06 μM 29628325
BL21(DE3) Function assay IC50 = 1.1 μM 19928858
K562 Antiproliferative activity assay IC50 = 1.22 μM 25778995
MDA-MB-231 Growth inhibition assay GI50 = 1.26 μM 28088086
MDA-MB-231 Cytotoxicity assay GI50 = 1.26 μM 26590508
MDA-MB-231 Antiproliferative activity assay GI50 = 1.26 μM 27017549
SK-MEL-28 Antiproliferative activity assay EC50 = 1.3 μM 18942827
sf9 Function assay Kd = 1.3 μM 28109791
F-6-8 Cytotoxicity assay IC50 = 1.3 μM 26318998
A549 Antiproliferative activity assay IC50 = 1.45 μM 26342134
rhabdomyosarcoma Antiviral activity assay EC50 = 1.5 μM 27288186
HL-60(TB) Growth inhibition assay GI50 = 1.58 μM 28088086
RPMI8226 Growth inhibition assay GI50 = 1.58 μM 28088086
KM12 Growth inhibition assay GI50 = 1.58 μM 28088086
LOXIMVI Growth inhibition assay GI50 = 1.58 μM 28088086
HCT116 Growth inhibition assay GI50 = 1.58 μM 28088086
HOP92 Growth inhibition assay GI50 = 1.58 μM 28088086
SF539 Growth inhibition assay GI50 = 1.58 μM 28088086
UACC62 Growth inhibition assay GI50 = 1.58 μM 28088086
SF295 Growth inhibition assay GI50 = 1.58 μM 28088086
MDA-MB-435 Growth inhibition assay GI50 = 1.58 μM 28088086
SK-MEL-5 Growth inhibition assay GI50 = 1.58 μM 28088086
T47D Growth inhibition assay GI50 = 1.58 μM 28088086
RPMI8266 Cytotoxicity assay GI50 = 1.58 μM 26590508
HL-60(TB) Cytotoxicity assay GI50 = 1.58 μM 26590508
KM12 Cytotoxicity assay GI50 = 1.58 μM 26590508
HCT116 Cytotoxicity assay GI50 = 1.58 μM 26590508
SF295 Cytotoxicity assay GI50 = 1.58 μM 26590508
SF539 Cytotoxicity assay GI50 = 1.58 μM 26590508
SK-MEL-2 Cytotoxicity assay GI50 = 1.58 μM 26590508
MDA-MB-435 Cytotoxicity assay GI50 = 1.58 μM 26590508
SK-MEL-5 Cytotoxicity assay GI50 = 1.58 μM 26590508
LOXIMVI Cytotoxicity assay GI50 = 1.58 μM 26590508
T47D Cytotoxicity assay GI50 = 1.58 μM 26590508
SMMC7721 Antiproliferative activity assay IC50 = 1.58 μM 26753815
LOXIMVI Antiproliferative activity assay GI50 = 1.58 μM 27017549
UACC62 Antiproliferative activity assay GI50 = 1.58 μM 27017549
SK-MEL-5 Antiproliferative activity assay GI50 = 1.58 μM 27017549
KM12 Antiproliferative activity assay GI50 = 1.58 μM 27017549
MDA-MB-435 Antiproliferative activity assay GI50 = 1.58 μM 27017549
SF539 Antiproliferative activity assay GI50 = 1.58 μM 27017549
SF295 Antiproliferative activity assay GI50 = 1.58 μM 27017549
HCT116 Antiproliferative activity assay GI50 = 1.58 μM 27017549
HOP92 Antiproliferative activity assay GI50 = 1.58 μM 27017549
RPMI8226 Antiproliferative activity assay GI50 = 1.58 μM 27017549
HL-60(TB) Antiproliferative activity assay GI50 = 1.58 μM 27017549
T47D Antiproliferative activity assay GI50 = 1.58 μM 27017549
7dF3 Function assay IC50 = 1.62 μM 29266937
MDA-MB-435 Antiproliferative activity assay IC50 = 1.67 μM 25778995
HL60 Cytotoxicity assay IC50 = 1.68 μM 24858546
SW579 Antiproliferative activity human IC50 = 1.73 μM 28242553
MCF7 Antiproliferative activity assay IC50 = 1.88 μM 25637123
A375P Antiproliferative activity assay IC50 = 1.9 μM 24128410
A549 Cytotoxicity assay IC50 = 1.92 μM 24826815
HCT116 Antiproliferative activity assay IC50 = 2 μM 22808911
MDA-MB-231 Cytotoxicity assay IC50 = 2 μM 23454017
NCI-H23 Growth inhibition assay GI50 = 2 μM 28088086
NCI-H522 Growth inhibition assay GI50 = 2 μM 28088086
HOP62 Growth inhibition assay GI50 = 2 μM 28088086
NCI-H226 Growth inhibition assay GI50 = 2 μM 28088086
HT-29 Growth inhibition assay GI50 = 2 μM 28088086
U251 Growth inhibition assay GI50 = 2 μM 28088086
COLO205 Growth inhibition assay GI50 = 2 μM 28088086
CCRF-CEM Growth inhibition assay GI50 = 2 μM 28088086
MALME-3M Growth inhibition assay GI50 = 2 μM 28088086
M14 Growth inhibition assay GI50 = 2 μM 28088086
UACC257 Growth inhibition assay GI50 = 2 μM 28088086
PC3 Growth inhibition assay GI50 = 2 μM 28088086
SK-MEL-2 Growth inhibition assay GI50 = 2 μM 28088086
MDA-MB-468 Growth inhibition assay GI50 = 2 μM 28088086
CCRF-CEM Cytotoxicity assay GI50 = 2 μM 26590508
NCI-H23 Cytotoxicity assay GI50 = 2 μM 26590508
NCI-H522 Cytotoxicity assay GI50 = 2 μM 26590508
COLO205 Cytotoxicity assay GI50 = 2 μM 26590508
HT-29 Cytotoxicity assay GI50 = 2 μM 26590508
SK-MEL-28 Cytotoxicity assay GI50 = 2 μM 26590508
HOP62 Cytotoxicity assay GI50 = 2 μM 26590508
UACC257 Cytotoxicity assay GI50 = 2 μM 26590508
NCI-H226 Cytotoxicity assay GI50 = 2 μM 26590508
U251 Cytotoxicity assay GI50 = 2 μM 26590508
PC3 Cytotoxicity assay GI50 = 2 μM 26590508
M14 Cytotoxicity assay GI50 = 2 μM 26590508
MDA-MB-468 Cytotoxicity assay GI50 = 2 μM 26590508
PC3 Antiproliferative activity assay GI50 = 2 μM 27017549
MALME-3M Antiproliferative activity assay GI50 = 2 μM 27017549
U251 Antiproliferative activity assay GI50 = 2 μM 27017549
UACC257 Antiproliferative activity assay GI50 = 2 μM 27017549
SK-MEL-2 Antiproliferative activity assay GI50 = 2 μM 27017549
COLO205 Antiproliferative activity assay GI50 = 2 μM 27017549
NCI-H23 Antiproliferative activity assay GI50 = 2 μM 27017549
HT-29 Antiproliferative activity assay GI50 = 2 μM 27017549
M14 Antiproliferative activity assay GI50 = 2 μM 27017549
NCI-H226 Antiproliferative activity assay GI50 = 2 μM 27017549
HOP62 Antiproliferative activity assay GI50 = 2 μM 27017549
MDA-MB-468 Antiproliferative activity assay GI50 = 2 μM 27017549
CCRF-CEM Antiproliferative activity assay GI50 = 2 μM 27017549
NCI-H522 Antiproliferative activity assay GI50 = 2 μM 27017549
A549 Antiproliferative activity assay IC50 = 2.02 μM 26753815
MDA-MB-435 Growth inhibition assay IC50 = 2.11 μM 29189002
NCI-H460 Antiproliferative activity assay IC50 = 2.19 μM 30216849
H460 Cytotoxicity assay IC50 = 2.19 μM 24826815
H460 Cytotoxicity assay IC50 = 2.19 μM 25086238
H460 Cytotoxicity assay IC50 = 2.19 μM 25440879
A375 Toxicity assay IC50 = 2.2 μM 19654408
H460 Antiproliferative activity assay IC50 = 2.25 μM 26991938
HCT116 Antiproliferative activity assay IC50 = 2.3 μM 23260578
MKN45 Antiproliferative activity assay IC50 = 2.32 μM 30216849
MKN45 Cytotoxicity assay IC50 = 2.32 μM 24826815
MKN45 Cytotoxicity assay IC50 = 2.32 μM 25086238
MKN45 Cytotoxicity assay IC50 = 2.32 μM 25440879
U937 Antiproliferative activity assay GI50 = 2.34 μM 29459144
A375 Antiproliferative activity assay IC50 = 2.4 μM 22808911
HeLa Growth inhibition assay IC50 = 2.44 μM 29102175
MDA-MB-231 Cytotoxicity assay IC50 = 2.5 μM 22414612
MCF7 Antiproliferative activity assay IC50 = 2.51 μM 30216849
UO31 Antiproliferative activity assay IC50 = 2.51 μM 30216849
NCI-H322M Growth inhibition assay GI50 = 2.51 μM 28088086
NCI-H460 Growth inhibition assay GI50 = 2.51 μM 28088086
KM12 Growth inhibition assay TGI = 2.51 μM 28088086
LOXIMVI Growth inhibition assay TGI = 2.51 μM 28088086
EKVX Growth inhibition assay GI50 = 2.51 μM 28088086
HCT116 Growth inhibition assay TGI = 2.51 μM 28088086
SW620 Growth inhibition assay GI50 = 2.51 μM 28088086
SF268 Growth inhibition assay GI50 = 2.51 μM 28088086
SF539 Growth inhibition assay TGI = 2.51 μM 28088086
A498 Growth inhibition assay GI50 = 2.51 μM 28088086
UACC62 Growth inhibition assay TGI = 2.51 μM 28088086
IGROV1 Growth inhibition assay GI50 = 2.51 μM 28088086
HCT15 Growth inhibition assay GI50 = 2.51 μM 28088086
SK-MEL-28 Growth inhibition assay GI50 = 2.51 μM 28088086
SK-MEL-28 Growth inhibition assay TGI = 2.51 μM 28088086
ACHN Growth inhibition assay GI50 = 2.51 μM 28088086
SK-MEL-5 Growth inhibition assay TGI = 2.51 μM 28088086
NCI/ADR-RES Growth inhibition assay GI50 = 2.51 μM 28088086
MCF7 Growth inhibition assay GI50 = 2.51 μM 28088086
SN12C Growth inhibition assay GI50 = 2.51 μM 28088086
Hs 578T Growth inhibition assay GI50 = 2.51 μM 28088086
SKOV3 Growth inhibition assay GI50 = 2.51 μM 28088086
UO31 Growth inhibition assay GI50 = 2.51 μM 28088086
NCI-H460 Cytotoxicity assay GI50 = 2.51 μM 26590508
HCT15 Cytotoxicity assay GI50 = 2.51 μM 26590508
SW620 Cytotoxicity assay GI50 = 2.51 μM 26590508
SF268 Cytotoxicity assay GI50 = 2.51 μM 26590508
IGROV1 Cytotoxicity assay GI50 = 2.51 μM 26590508
OVCAR8 Cytotoxicity assay GI50 = 2.51 μM 26590508
NCI/ADR-RES Cytotoxicity assay GI50 = 2.51 μM 26590508
SKOV3 Cytotoxicity assay GI50 = 2.51 μM 26590508
SN12C Cytotoxicity assay GI50 = 2.51 μM 26590508
NCI-H322M Cytotoxicity assay GI50 = 2.51 μM 26590508
MCF7 Cytotoxicity assay GI50 = 2.51 μM 26590508
UO31 Cytotoxicity assay GI50 = 2.51 μM 26590508
Hs578T Cytotoxicity assay GI50 = 2.51 μM 26590508
A498 Cytotoxicity assay GI50 = 2.51 μM 26590508
A498 Antiproliferative activity assay GI50 = 2.51 μM 27017549
SKOV3 Antiproliferative activity assay GI50 = 2.51 μM 27017549
UO31 Antiproliferative activity assay GI50 = 2.51 μM 27017549
NCI-ADR-RES Antiproliferative activity assay GI50 = 2.51 μM 27017549
SN12C Antiproliferative activity assay GI50 = 2.51 μM 27017549
IGROV1 Antiproliferative activity assay GI50 = 2.51 μM 27017549
ACHN Antiproliferative activity assay GI50 = 2.51 μM 27017549
OVCAR8 Antiproliferative activity assay GI50 = 2.51 μM 27017549
SK-MEL-28 Antiproliferative activity assay GI50 = 2.51 μM 27017549
NCI-H322M Antiproliferative activity assay GI50 = 2.51 μM 27017549
SF268 Antiproliferative activity assay GI50 = 2.51 μM 27017549
HCT15 Antiproliferative activity assay GI50 = 2.51 μM 27017549
NCI-H460 Antiproliferative activity assay GI50 = 2.51 μM 27017549
SW620 Antiproliferative activity assay GI50 = 2.51 μM 27017549
EKVX Antiproliferative activity assay GI50 = 2.51 μM 27017549
MCF7 Antiproliferative activity assay GI50 = 2.51 μM 27017549
Hs 578T Antiproliferative activity assay GI50 = 2.51 μM 27017549
HT-29 Antiproliferative activity assay IC50 = 2.58 μM 29886324
A375P Antiproliferative activity assay GI50 = 2.58 μM 26810260
TPC1 Antiproliferative activity assay EC50 = 2.6 μM 22559926
Hep3B Growth inhibition assay IC50 = 2.63 μM 29102175
A375P Antiproliferative activity assay IC50 = 2.7 μM 22460030
U937 Antiproliferative activity assay GI50 = 2.74 μM 26318067
U937 Cytotoxicity assay GI50 = 2.74 μM 24878193
MCF7 Growth inhibition assay IC50 = 2.78 μM 29102175
MDA-MB-231 Antiproliferative activity assay IC50 = 2.8 μM 29202403
HepG2 Antiproliferative activity assay IC50 = 2.84 μM 28242553
U937 Growth inhibition assay GI50 = 2.85 μM 22014755
A549 Cytotoxicity assay IC50 = 2.92 μM 28927801
A549 Cytotoxicity assay IC50 = 2.92 μM 27777009
ZR75-30 Growth inhibition assay IC50 = 2.96 μM 29102175
PC3 Cytotoxicity assay IC50 = 3.03 μM 28340913
MDA-MB-231 Antiproliferative activity assay IC50 = 3.08 μM 26991938
A549 Growth inhibition assay IC50 = 3.1 μM 29102175
K562 Growth inhibition assay GI50 = 3.16 μM 28088086
MOLT4 Growth inhibition assay GI50 = 3.16 μM 28088086
A549/ATCC Growth inhibition assay GI50 = 3.16 μM 28088086
RPMI8226 Growth inhibition assay TGI = 3.16 μM 28088086
SR Growth inhibition assay GI50 = 3.16 μM 28088086
HOP62 Growth inhibition assay TGI = 3.16 μM 28088086
NCI-H226 Growth inhibition assay TGI = 3.16 μM 28088086
U251 Growth inhibition assay TGI = 3.16 μM 28088086
COLO205 Growth inhibition assay TGI = 3.16 μM 28088086
M14 Growth inhibition assay TGI = 3.16 μM 28088086
HCC2998 Growth inhibition assay GI50 = 3.16 μM 28088086
SNB75 Growth inhibition assay GI50 = 3.16 μM 28088086
786-0 Growth inhibition assay GI50 = 3.16 μM 28088086
A498 Growth inhibition assay TGI = 3.16 μM 28088086
HCT15 Growth inhibition assay TGI = 3.16 μM 28088086
OVCAR3 Growth inhibition assay GI50 = 3.16 μM 28088086
OVCAR4 Growth inhibition assay GI50 = 3.16 μM 28088086
Caki1 Growth inhibition assay GI50 = 3.16 μM 28088086
SNB19 Growth inhibition assay GI50 = 3.16 μM 28088086
OVCAR5 Growth inhibition assay GI50 = 3.16 μM 28088086
DU145 Growth inhibition assay GI50 = 3.16 μM 28088086
OVCAR8 Growth inhibition assay GI50 = 3.16 μM 28088086
SN12C Growth inhibition assay TGI = 3.16 μM 28088086
MDA-MB-231 Growth inhibition assay TGI = 3.16 μM 28088086
RXF393 Growth inhibition assay GI50 = 3.16 μM 28088086
BT549 Growth inhibition assay GI50 = 3.16 μM 28088086
K562 Cytotoxicity assay GI50 = 3.16 μM 26590508
MOLT4 Cytotoxicity assay GI50 = 3.16 μM 26590508
SNB19 Cytotoxicity assay GI50 = 3.16 μM 26590508
SR Cytotoxicity assay GI50 = 3.16 μM 26590508
A549 Cytotoxicity assay GI50 = 3.16 μM 26590508
OVCAR3 Cytotoxicity assay GI50 = 3.16 μM 26590508
OVCAR4 Cytotoxicity assay GI50 = 3.16 μM 26590508
SNB75 Cytotoxicity assay GI50 = 3.16 μM 26590508
OVCAR5 Cytotoxicity assay GI50 = 3.16 μM 26590508
DU145 Cytotoxicity assay GI50 = 3.16 μM 26590508
786-0 Cytotoxicity assay GI50 = 3.16 μM 26590508
BT549 Cytotoxicity assay GI50 = 3.16 μM 26590508
ACHN Cytotoxicity assay GI50 = 3.16 μM 26590508
Caki1 Cytotoxicity assay GI50 = 3.16 μM 26590508
786-0 Antiproliferative activity assay GI50 = 3.16 μM 27017549
LOXIMVI Antiproliferative activity assay TGI = 3.16 μM 27017549
Caki1 Antiproliferative activity assay GI50 = 3.16 μM 27017549
OVCAR5 Antiproliferative activity assay GI50 = 3.16 μM 27017549
RXF393 Antiproliferative activity assay GI50 = 3.16 μM 27017549
SNB75 Antiproliferative activity assay GI50 = 3.16 μM 27017549
OVCAR3 Antiproliferative activity assay GI50 = 3.16 μM 27017549
SNB19 Antiproliferative activity assay GI50 = 3.16 μM 27017549
SK-MEL-5 Antiproliferative activity assay TGI = 3.16 μM 27017549
OVCAR4 Antiproliferative activity assay GI50 = 3.16 μM 27017549
SK-MEL-2 Antiproliferative activity assay TGI = 3.16 μM 27017549
BT549 Antiproliferative activity assay GI50 = 3.16 μM 27017549
MOLT4 Antiproliferative activity assay GI50 = 3.16 μM 27017549
K562 Antiproliferative activity assay GI50 = 3.16 μM 27017549
HCC2998 Antiproliferative activity assay GI50 = 3.16 μM 27017549
HCC2998 Antiproliferative activity assay TGI = 3.16 μM 27017549
A549/ATCC Antiproliferative activity assay GI50 = 3.16 μM 27017549
DU145 Antiproliferative activity assay GI50 = 3.16 μM 27017549
SR Antiproliferative activity assay GI50 = 3.16 μM 27017549
MCF7 Cytotoxicity assay IC50 = 3.18 μM 28927801
PC3 Cytotoxicity assay IC50 = 3.18 μM 28927801
MCF7 Cytotoxicity assay IC50 = 3.18 μM 27777009
A549 Antiproliferative activity assay IC50 = 3.19 μM 25778995
PC3 Cytotoxicity assay IC50 = 3.24 μM 27777009
HeLa Function assay IC50 = 3.3 μM 15225706
HeLa Function assay IC50 = 3.3 μM 15225706
LoVo Cytotoxicity assay IC50 = 3.3 μM 23454017
A375 Antiproliferative activity assay IC50 = 3.36 μM 29602674
HT-29 Antiproliferative activity assay IC50 = 3.37 μM 26991938
FLT3 gene-deficient U937 Antiproliferative activity assay GI50 = 3.4 μM 21708468
FLT3 negative U937 Cytotoxicity assay GI50 = 3.4 μM 23618709
U937 Cytotoxicity assay GI50 = 3.4 μM 26081023
A375P Antiproliferative activity assay GI50 = 3.4 μM 29459144
ACHN Cytotoxicity assay IC50 = 3.4 μM 29517908
ACHN Cytotoxicity assay IC50 = 3.4 μM 29297688
HepG2 Function assay IC50 = 3.4 μM 26071861
A375P Cytotoxicity assay GI50 = 3.4 μM 24878193
HepG2 Cytotoxicity assay IC50 = 3.44 μM 28927801
HepG2 Cytotoxicity assay IC50 = 3.44 μM 27777009
ACHN Cytotoxicity assay IC50 = 3.5 μM 29786436
HepG2 Antiproliferative activity assay IC50 = 3.5 μM 25462265
HT-29 Cytotoxicity assay IC50 = 3.61 μM 24826815
HT-29 Antiproliferative activity assay IC50 = 3.61 μM 30216849
HT-29 Cytotoxicity assay IC50 = 3.61 μM 25086238
HT-29 Cytotoxicity assay IC50 = 3.61 μM 25440879
MCF7 Anticancer activity assay IC50 = 3.64 μM 29549841
Sf9 Function assay IC50 = 3.8 μM 21708468
Sf9 Function assay IC50 = 3.8 μM 23618709
Sf9 Function assay IC50 = 3.8 μM 26081023
A2058 Cytotoxicity assay IC50 = 3.8 μM 22708987
NCI-H460 Cytotoxicity assay IC50 = 3.9 μM 23454017
SK-MEL-30 Cytotoxicity assay IC50 = 3.9 μM 29461827
HT-29 Anticancer activity assay IC50 = 3.97 μM 29549841
SF268 Growth inhibition assay TGI = 3.98 μM 28088086
SNB75 Growth inhibition assay TGI = 3.98 μM 28088086
OVCAR3 Growth inhibition assay TGI = 3.98 μM 28088086
SNB19 Growth inhibition assay TGI = 3.98 μM 28088086
Hs 578T Growth inhibition assay TGI = 3.98 μM 28088086
TK10 Growth inhibition assay GI50 = 3.98 μM 28088086
BT549 Growth inhibition assay TGI = 3.98 μM 28088086
Caki1 Antiproliferative activity assay TGI = 3.98 μM 27017549
TK10 Antiproliferative activity assay GI50 = 3.98 μM 27017549
MDA-MB-435 Antiproliferative activity assay TGI = 3.98 μM 27017549
HCT116 Antiproliferative activity assay TGI = 3.98 μM 27017549
MDA-MB-231 Antiproliferative activity assay TGI = 3.98 μM 27017549
HepG2 Cytotoxicity assay IC50 = 4 μM 23454017
HT-29 Cytotoxicity assay IC50 = 4 μM 23454017
A549 Cytotoxicity assay IC50 = 4 μM 23454017
HuH7 Cytotoxicity assay GI50 = 4 μM 23726028
PC3 Antiproliferative activity assay IC50 = 4.13 μM 25778995
HeLa Cytotoxicity assay IC50 = 4.163 μM 23362959
MDA-MB-436 Antiproliferative activity assay IC50 = 4.2 μM 29202403
MCF7 Cytotoxicity assay IC50 = 4.21 μM 27043268
MCF7 Cytotoxicity assay IC50 = 4.21 μM 28340913
LOXIMVI Antiproliferative activity assay IC50 = 4.25 μM 25778995
OVCAR4 Cytotoxicity assay TGI = 4.31 μM 26590508
WM1361 Antiproliferative activity assay GI50 = 4.345 μM 20148563
WM266.4 Growth inhibition assay GI50 = 4.5 μM 20199087
HepG2 Cytotoxicity assay GI50 = 4.5 μM 23726028
A549 Antiproliferative activity assay IC50 = 4.5 μM 23260578
LS174T Function assay IC50 = 4.52 μM 29266937
8505C Antiproliferative activity assay IC50 = 4.7 μM 29032031
OVCAR8 Cytotoxicity assay TGI = 4.73 μM 26590508
MDA-MB-231 Cytotoxicity assay IC50 = 4.77 μM 20435479
B16-F1 Antiproliferative activity assay IC50 = 4.9 μM 18477505
WM164 Antiproliferative activity assay IC50 = 4.9 μM 17561392
B16-F1 Antiproliferative activity assay IC50 = 4.9 μM 20056548
MDA-MB-468 Cytotoxicity assay IC50 = 4.9 μM 26159483
786-O Cytotoxicity assay IC50 = 4.9 μM 29517908
786-O Cytotoxicity assay IC50 = 4.9 μM 29297688
WM266.4 Antiproliferative activity assay GI50 = 4.933 μM 20148563
WM266.4 Growth inhibition assay IC50 = 5 μM 19323560
WM164 Antiproliferative activity assay IC50 = 5 μM 20056548
HepG2 Antiproliferative activity assay IC50 = 5 μM 23260578
HepG2 Antiproliferative activity assay IC50 = 5 μM 23932071
NCI-H23 Growth inhibition assay TGI = 5.01 μM 28088086
NCI-H322M Growth inhibition assay TGI = 5.01 μM 28088086
NCI-H460 Growth inhibition assay TGI = 5.01 μM 28088086
NCI-H522 Growth inhibition assay TGI = 5.01 μM 28088086
HT-29 Growth inhibition assay TGI = 5.01 μM 28088086
CCRF-CEM Growth inhibition assay TGI = 5.01 μM 28088086
SW620 Growth inhibition assay TGI = 5.01 μM 28088086
HOP92 Growth inhibition assay TGI = 5.01 μM 28088086
786-0 Growth inhibition assay TGI = 5.01 μM 28088086
MDA-MB-435 Growth inhibition assay TGI = 5.01 μM 28088086
PC3 Growth inhibition assay TGI = 5.01 μM 28088086
UACC257 Growth inhibition assay TGI = 5.01 μM 28088086
SKOV3 Growth inhibition assay TGI = 5.01 μM 28088086
RXF393 Growth inhibition assay TGI = 5.01 μM 28088086
T47D Growth inhibition assay TGI = 5.01 μM 28088086
MDA-MB-468 Growth inhibition assay TGI = 5.01 μM 28088086
UACC62 Antiproliferative activity assay TGI = 5.01 μM 27017549
UACC257 Antiproliferative activity assay TGI = 5.01 μM 27017549
SK-MEL-5 Antiproliferative activity assay LC50 = 5.01 μM 27017549
M14 Antiproliferative activity assay TGI = 5.01 μM 27017549
NCI-H23 Antiproliferative activity assay TGI = 5.01 μM 27017549
SF295 Antiproliferative activity assay TGI = 5.01 μM 27017549
HOP92 Antiproliferative activity assay TGI = 5.01 μM 27017549
BT549 Antiproliferative activity assay TGI = 5.01 μM 27017549
MDA-MB-231 Cytotoxicity assay IC50 = 5.1 μM 26159483
DU145 Cytotoxicity assay IC50 = 5.1 μM 22708987
A549 Cytotoxicity assay IC50 = 5.21 μM 20181414
HeLa Cytotoxicity assay IC50 = 5.23 μM 26342867
786-O Cytotoxicity assay IC50 = 5.3 μM 29786436
HCT116 Antiproliferative activity assay GI50 = 5.4 μM 15225706
A375 Antiproliferative activity assay IC50 = 5.4 μM 18477505
SK-MEL-188 Antiproliferative activity assay IC50 = 5.4 μM 17561392
A375 Antiproliferative activity assay IC50 = 5.4 μM 20056548
MCF7 Cytotoxicity assay IC50 = 5.5 μM 26159483
A375 Antiproliferative activity assay IC50 = 5.58 μM 19464887
A375P Cytotoxicity assay IC50 = 5.58 μM 20797858
A375P Antiproliferative activity assay GI50 = 5.58 μM 21353571
A375P Growth inhibition assay GI50 = 5.58 μM 22014755
A375P Growth inhibition assay GI50 = 5.58 μM 20149658
A375P Antiproliferative activity assay GI50 = 5.58 μM 20466542
A375P Antiproliferative activity assay IC50 = 5.6 μM 19857963
A375P Antiproliferative activity assay IC50 = 5.6 μM 21592628
A375P Antiproliferative activity assay IC50 = 5.6 μM 22033063
A375P Cytotoxicity assay IC50 = 5.6 μM 19897366
A375P Antiproliferative activity assay IC50 = 5.6 μM 22647720
HCT116 Cytotoxicity assay IC50 = 5.65 μM 24215818
SH-SY5Y Antiproliferative activity assay IC50 = 5.73 μM 24315192
HepG2 Cytotoxicity assay IC50 = 5.74 μM 25461318
Bel7402 Cytotoxicity assay IC50 = 5.8 μM 23454017
HT-29 Cytotoxicity assay IC50 = 5.9 μM 28865276
melanoma Growth inhibition assay IC50 = 6.1 μM 16392826
K562 Antiproliferative activity assay GI50 = 6.2 μM 21708468
HepG2 Cytotoxicity assay IC50 = 6.2 μM 28865276
A549 Anticancer activity assay IC50 = 6.21 μM 29549841
SMMC7721 Antiproliferative activity assay IC50 = 6.23 μM 22721924
HepG2 Antiproliferative activity assay IC50 = 6.3 μM 23932071
SF295 Growth inhibition assay TGI = 6.31 μM 28088086
SK-MEL-2 Growth inhibition assay TGI = 6.31 μM 28088086
OVCAR5 Growth inhibition assay TGI = 6.31 μM 28088086
UO31 Growth inhibition assay TGI = 6.31 μM 28088086
A498 Antiproliferative activity assay TGI = 6.31 μM 27017549
MALME-3M Antiproliferative activity assay TGI = 6.31 μM 27017549
U251 Antiproliferative activity assay TGI = 6.31 μM 27017549
SK-MEL-2 Antiproliferative activity assay LC50 = 6.31 μM 27017549
RPMI8226 Antiproliferative activity assay TGI = 6.31 μM 27017549
HCC2998 Antiproliferative activity assay LC50 = 6.31 μM 27017549
NCI-H522 Antiproliferative activity assay TGI = 6.31 μM 27017549
HUVEC Antiproliferative activity assay IC50 = 6.42 μM 23644219
A549 Cytotoxicity assay IC50 = 6.53 μM 27043268
A549 Cytotoxicity assay IC50 = 6.53 μM 28340913
LoVo Antiproliferative activity assay IC50 = 6.56 μM 24315192
A375 Function assay IC50 = 6.599 μM 21807507
HCT116 Function assay GI50 = 6.6 μM 15225706
HepG2 Cytotoxicity assay IC50 = 6.7 μM 26159483
BCPAP Antiproliferative activity assay IC50 = 6.7 μM 29032031
A549 Cytotoxicity assay IC50 = 6.7 μM 28865276
PC3 Cytotoxicity assay IC50 = 6.8 μM 23021967
SGC7901 Cytotoxicity assay IC50 = 6.9 μM 23454017
OS-RC2 Cytotoxicity assay IC50 = 7 μM 29517908
OS-RC2 Cytotoxicity assay IC50 = 7 μM 29297688
COLO205 Antiproliferative activity human IC50 = 7.04 μM 28242553
rhabdomyosarcoma Cytotoxicity activity against human CC50 = 7.05 μM 27288186
HuH7 Cytotoxicity assay IC50 = 7.1 μM 26159483
MDA-MB-231 Antiproliferative activity assay IC50 = 7.18 μM 22721924
FLT3-negative K562 Cytotoxicity assay GI50 = 7.3 μM 23618709
K562 Function assay GI50 = 7.3 μM 26081023
K562 Function assay GI50 = 7.3 μM 26081023
MCF7 Antiproliferative activity assay IC50 = 7.33 μM 23644219
A549 Cytotoxicity assay TGI = 7.36 μM 26590508
WI38 Cytotoxicity assay IC50 = 7.54 μM 24826815
A375 Cytotoxicity assay IC50 = 7.56 μM 24215818
MDA-MB-231 Cytotoxicity assay IC50 = 7.62 μM 20181414
786-0 Cytotoxicity assay TGI = 7.62 μM 26590508
HS27 Antiproliferative activity assay IC50 = 7.8 μM 19857963
HS27 Cytotoxicity assay IC50 = 7.8 μM 19897366
HCT116 Cytotoxicity assay IC50 = 7.8 μM 22483592
HS27 Antiproliferative activity assay IC50 = 7.85 μM 19464887
HS27 Antiproliferative activity assay GI50 = 7.85 μM 21353571
A549/ATCC Growth inhibition assay TGI = 7.94 μM 28088086
DU145 Growth inhibition assay TGI = 7.94 μM 28088086
NCI/ADR-RES Growth inhibition assay TGI = 7.94 μM 28088086
MCF7 Growth inhibition assay TGI = 7.94 μM 28088086
PC3 Antiproliferative activity assay TGI = 7.94 μM 27017549
UO31 Antiproliferative activity assay TGI = 7.94 μM 27017549
NCI-ADR-RES Antiproliferative activity assay TGI = 7.94 μM 27017549
LOXIMVI Antiproliferative activity assay LC50 = 7.94 μM 27017549
SK-MEL-28 Antiproliferative activity assay TGI = 7.94 μM 27017549
KM12 Antiproliferative activity assay TGI = 7.94 μM 27017549
COLO205 Antiproliferative activity assay TGI = 7.94 μM 27017549
HT-29 Antiproliferative activity assay TGI = 7.94 μM 27017549
NCI-H226 Antiproliferative activity assay TGI = 7.94 μM 27017549
HOP62 Antiproliferative activity assay TGI = 7.94 μM 27017549
T47D Antiproliferative activity assay TGI = 7.94 μM 27017549
MDA-MB-468 Antiproliferative activity assay TGI = 7.94 μM 27017549
EKVX Antiproliferative activity assay TGI = 7.94 μM 27017549
MCF7 Antiproliferative activity assay TGI = 7.94 μM 27017549
Hs 578T Antiproliferative activity assay TGI = 7.94 μM 27017549
MGC803 Antiproliferative activity assay IC50 = 7.99 μM 26560049
HCT116 Antiproliferative activity assay IC50 = 8.08 μM 24440479
PC3 Cytotoxicity assay IC50 = 8.08 μM 27043268
HCT116 Antiproliferative activity assay IC50 = 8.08 μM 23644219
WM266.4 Antiproliferative activity assay GI50 = 8.1 μM 23025996
WM266.4 Antiproliferative activity assay GI50 = 8.12 μM 22583669
Ketr3 Antiproliferative activity assay IC50 = 8.27 μM 30216849
A375 Antiproliferative activity assay IC50 = 8.27 μM 30216849
HepG2 Antiproliferative activity assay IC50 = 8.27 μM 30216849
MX1 Antiproliferative activity assay IC50 = 8.27 μM 30216849
MX1 Cytotoxicity assay IC50 = 8.27 μM 24675135
WM266.4 Growth inhibition assay GI50 = 8.3 μM 22361686
PLC/PRF/5 Cytotoxicity assay IC50 = 8.3 μM 21531053
A375 Antiproliferative activity assay IC50 = 8.33 μM 29886324
HCT116 Cytotoxicity assay IC50 = 8.41 μM 29631788
WI38 Cytotoxicity assay IC50 = 8.42 μM 26991938
HepG2 Cytotoxicity assay IC50 = 8.42 μM 27162123
HepG2 Cytotoxicity assay IC50 = 8.42 μM 23871909
HT-29 Antiproliferative activity assay IC50 = 8.44 μM 29602674
HepG2 Cytotoxicity assay IC50 = 8.67 μM 24675135
MCF7 Cytotoxicity assay IC50 = 8.83 μM 20435479
MCF7 Cytotoxicity assay IC50 = 9.12 μM 24300920
HepG2 Antiproliferative activity assay IC50 = 9.14 μM 26560049
A375 Cytotoxicity assay IC50 = 9.17 μM 24675135
MGC803 Antiproliferative activity assay IC50 = 9.2 μM 29032031
SKOV3 Cytotoxicity assay IC50 = 9.25 μM 24300920
RS4:11 Function assay GI50 = 9.3 μM 26081023
RS4:11 Cytotoxicity assay GI50 = 9.3 μM 23618709
MIAPaCa2 Antiproliferative activity assay IC50 = 9.32 μM 29032031
PANC1 Growth inhibition assay IC50 = 9.32 μM 29102175
MHCC97H Growth inhibition assay IC50 = 9.32 μM 29102175
RS4:11 Antiproliferative activity assay GI50 = 9.4 μM 21708468
Hep3B Cytotoxicity assay IC50 = 9.4 μM 28865276
LoVo Growth inhibition assay IC50 = 9.47 μM 29102175
SMMC7721 Antiproliferative activity assay IC50 = 9.96 μM 25637123
MCF7 Cytotoxicity assay TGI = 9.97 μM 26590508
IGROV1 Growth inhibition assay TGI = 10 μM 28088086
ACHN Growth inhibition assay TGI = 10 μM 28088086
TK10 Growth inhibition assay TGI = 10 μM 28088086
786-0 Antiproliferative activity assay TGI = 10 μM 27017549
SN12C Antiproliferative activity assay TGI = 10 μM 27017549
Caki1 Antiproliferative activity assay LC50 = 10 μM 27017549
TK10 Antiproliferative activity assay TGI = 10 μM 27017549
RXF393 Antiproliferative activity assay TGI = 10 μM 27017549
OVCAR8 Antiproliferative activity assay TGI = 10 μM 27017549
SNB75 Antiproliferative activity assay TGI = 10 μM 27017549
NCI-H322M Antiproliferative activity assay TGI = 10 μM 27017549
MDA-MB-435 Antiproliferative activity assay LC50 = 10 μM 27017549
SF539 Antiproliferative activity assay TGI = 10 μM 27017549
SF268 Antiproliferative activity assay TGI = 10 μM 27017549
NCI-H460 Antiproliferative activity assay TGI = 10 μM 27017549
DU145 Antiproliferative activity assay TGI = 10 μM 27017549
K1 Antiproliferative activity assay IC50 = 10.2 μM 29032031
Bel7402 Cytotoxicity assay IC50 = 10.26 μM 21504204
Bel7402 Growth inhibition assay IC50 = 10.31 μM 29102175
OVCAR3 Cytotoxicity assay TGI = 10.32 μM 26590508
SGC7901 Cytotoxicity assay IC50 = 10.37 μM 20435479
SNB75 Cytotoxicity assay TGI = 10.42 μM 26590508
A431 Antiproliferative activity assay IC50 = 10.46 μM 29032031
SMMC7721 Antiproliferative activity assay IC50 = 10.61 μM 29032031
GES-1 Cytotoxicity assay IC50 = 10.68 μM 27162123
H460 Cytotoxicity assay IC50 = 10.8 μM 24300920
BGC823 Antiproliferative activity assay IC50 = 10.91 μM 22721924
Hep3B Cytotoxicity assay IC50 = 11.2 μM 28342400
MCF7 Cytotoxicity assay IC50 = 11.34 μM 27162123
MCF7 Cytotoxicity assay IC50 = 11.34 μM 23871909
SK-MEL-2 Antiproliferative activity human IC50 = 11.35 μM 28242553
HepG2 Cytotoxicity assay IC50 = 11.49 μM 21504204
A375P Antiproliferative activity assay IC50 = 11.5 μM 22014559
SGC7901 Cytotoxicity assay IC50 = 11.5 μM 24300920
HeLa Antiproliferative activity assay IC50 = 12.01 μM 29103873
PANC1 Cytotoxicity assay IC50 = 12.3 μM 24300920
HepG2 Antiproliferative activity assay IC50 = 12.54 μM 29032031
A549 Antiproliferative activity assay IC50 = 12.54 μM 23644219
Caki1 Growth inhibition assay TGI = 12.59 μM 28088086
OVCAR8 Growth inhibition assay TGI = 12.59 μM 28088086
SKOV3 Antiproliferative activity assay TGI = 12.6 μM 27017549
ACHN Antiproliferative activity assay TGI = 12.6 μM 27017549
OVCAR3 Antiproliferative activity assay TGI = 12.6 μM 27017549
OVCAR4 Antiproliferative activity assay TGI = 12.6 μM 27017549
HCT15 Antiproliferative activity assay TGI = 12.6 μM 27017549
SW620 Antiproliferative activity assay TGI = 12.6 μM 27017549
A549/ATCC Antiproliferative activity assay TGI = 12.6 μM 27017549
MDA-MB-468 Cytotoxicity assay TGI = 13.09 μM 26590508
SK-MEL-28 Cytotoxicity assay TGI = 13.39 μM 26590508
A549 Antiproliferative activity assay IC50 = 13.64 μM 26560049
A375 Antiproliferative activity human IC50 = 13.64 μM 28242553
A375 Antiproliferative activity assay IC50 = 13.64 μM 25462267
K562 Antiproliferative activity assay IC50 = 13.85 μM 23644219
Hep3B Cytotoxicity assay IC50 = 14.08 μM 21504204
T47D Cytotoxicity assay TGI = 14.38 μM 26590508
NCI-H226 Cytotoxicity assay TGI = 14.42 μM 26590508
MDA-MB-231 Antiproliferative activity assay IC50 = 14.62 μM 24440479
MDA-MB-231 Antiproliferative activity assay IC50 = 14.62 μM 23644219
NCI-H522 Cytotoxicity assay TGI = 14.82 μM 26590508
SK-MEL-2 Cytotoxicity assay TGI = 14.85 μM 26590508
OS-RC2 Cytotoxicity assay IC50 = 15 μM 29786436
HepG2 Antiproliferative activity assay IC50 = 15 μM 29103873
fibroblast Antiproliferative activity assay IC50 = 15.1 μM 18477505
HT-29 Cytotoxicity assay IC50 = 15.2 μM 24675135
U87MG Cytotoxicity assay IC50 = 15.57 μM 24826815
BT549 Antiproliferative activity assay LC50 = 15.8 μM 27017549
GES-1 Cytotoxicity assay IC50 = 15.8 μM 23871909
SNB19 Antiproliferative activity assay TGI = 15.85 μM 27017549
IGROV1 Antiproliferative activity assay TGI = 15.9 μM 27017549
HCT116 Antiproliferative activity assay LC50 = 15.9 μM 27017549
OS-RC2 Cytotoxicity assay IC50 = 16 μM 23454017
A375 Cytotoxicity assay IC50 = 16.24 μM 25461318
SKOV3 Cytotoxicity assay TGI = 16.36 μM 26590508
WM1361 Antiproliferative activity assay IC50 = 16.44 μM 29602674
MKN28 Antiproliferative activity assay IC50 = 17 μM 29032031
SMMC7721 Cytotoxicity assay IC50 = 17.3 μM 21504204
UACC257 Cytotoxicity assay TGI = 17.33 μM 26590508
EAhy926 Antiangiogenic activity assay IC50 = 18.52 μM 29032031
SMMC7721 Cytotoxicity assay IC50 = 18.7 μM 24300920
Ketr3 Cytotoxicity assay IC50 = 18.8 μM 24675135
NCI-H522 Cytotoxicity assay IC50 = 19.26 μM 25461318
A549 Cytotoxicity assay IC50 = 19.54 μM 27162123
SH-SY5Y Cytotoxicity assay IC50 = 19.54 μM 23871909
MGC803 Antiproliferative activity assay IC50 = 19.92 μM 29103873
EKVX Growth inhibition assay TGI = 19.95 μM 28088086
OVCAR5 Antiproliferative activity assay TGI = 20 μM 27017549
UACC62 Antiproliferative activity assay LC50 = 20 μM 27017549
UACC257 Antiproliferative activity assay LC50 = 20 μM 27017549
MDA-MB-231 Antiproliferative activity assay LC50 = 20 μM 27017549
U87 Cytotoxicity assay IC50 = 21.07 μM 20435479
EJ Cytotoxicity assay IC50 = 22.9 μM 24300920
HCT116 Antiproliferative activity assay IC50 = 23.31 μM 29602674
HOP62 Cytotoxicity assay TGI = 23.55 μM 26590508
MDA-MB-231 Cytotoxicity assay TGI = 23.93 μM 26590508
PC3 Antiproliferative activity assay IC50 = 24.2 μM 24440479
PC3 Antiproliferative activity assay IC50 = 24.2 μM 23644219
EAhy926 Antiproliferative activity assay IC50 = 24.36 μM 28068599
EAhy926 Anti-angiogenic activity in human IC50 = 24.36 μM 29102175
U251 Cytotoxicity assay IC50 = 24.71 μM 20435479
NIH/3T3 Antiproliferative activity assay IC50 = 24.75 μM 21592628
NIH/3T3 Antiproliferative activity assay IC50 = 24.75 μM 22647720
DU145 Cytotoxicity assay IC50 = 24.91 μM 27162123
DU145 Cytotoxicity assay IC50 = 24.91 μM 23871909
U251 Antiproliferative activity assay LC50 = 25.1 μM 27017549
M14 Antiproliferative activity assay LC50 = 25.1 μM 27017549
NCI-H522 Antiproliferative activity assay LC50 = 25.1 μM 27017549
OVCAR4 Growth inhibition assay TGI = 25.12 μM 28088086
SH-SY5Y Cytotoxicity assay IC50 = 27.71 μM 27162123
A549 Cytotoxicity assay IC50 = 27.71 μM 23871909
PLC/PRF/5 Cytotoxicity assay IC50 = 29.9 μM 28109948
SK-MEL-5 Cytotoxicity assay TGI = 31.26 μM 26590508
A498 Antiproliferative activity assay LC50 = 31.6 μM 27017549
SK-MEL-28 Antiproliferative activity assay LC50 = 31.6 μM 27017549
KM12 Antiproliferative activity assay LC50 = 31.6 μM 27017549
COLO205 Antiproliferative activity assay LC50 = 31.6 μM 27017549
NCI-H226 Antiproliferative activity assay LC50 = 31.6 μM 27017549
SF295 Antiproliferative activity assay LC50 = 31.6 μM 27017549
HOP62 Antiproliferative activity assay LC50 = 31.6 μM 27017549
T47D Antiproliferative activity assay LC50 = 31.6 μM 27017549
MHCC97L Cytotoxicity assay IC50 = 34.41 μM 28109948
MDA-MB-231 Antiproliferative activity assay IC50 = 35 μM 24315192
MDA-MB-231 Cytotoxicity assay IC50 = 36 μM 22483592
B16-BL6 Cytotoxicity assay IC50 = 36.48 μM 29631788
UO31 Antiproliferative activity assay LC50 = 39.8 μM 27017549
SN12C Antiproliferative activity assay LC50 = 39.8 μM 27017549
RXF393 Antiproliferative activity assay LC50 = 39.8 μM 27017549
SNB75 Antiproliferative activity assay LC50 = 39.8 μM 27017549
SF268 Antiproliferative activity assay LC50 = 39.8 μM 27017549
NCI-H23 Antiproliferative activity assay LC50 = 39.8 μM 27017549
HT-29 Antiproliferative activity assay LC50 = 39.8 μM 27017549
HOP92 Antiproliferative activity assay LC50 = 39.8 μM 27017549
NCI-H460 Antiproliferative activity assay LC50 = 39.8 μM 27017549
SW620 Antiproliferative activity assay LC50 = 39.8 μM 27017549
MDA-MB-468 Antiproliferative activity assay LC50 = 39.8 μM 27017549
MALME-3M Growth inhibition assay TGI = 39.81 μM 28088086
클릭하여 더 많은 세포주 실험 데이터 보기

화학 정보, 보관 및 안정성 (Chemical Information, Storage & Stability)

분자량 464.82 화학식

C21H16ClF3N4O3

 보관 (수령일로부터)
CAS 번호 284461-73-0 SDF 다운로드 원액 보관

동의어 NSC-724772,BAY 43-9006 Smiles CNC(=O)C1=NC=CC(=C1)OC2=CC=C(C=C2)NC(=O)NC3=CC(=C(C=C3)Cl)C(F)(F)F

용해도 (Solubility)

In vitro
배치:

DMSO : 92 mg/mL (197.92 mM)
(수분으로 오염된 DMSO는 용해도를 감소시킬 수 있습니다. 신선하고 무수 DMSO를 사용하십시오.)

Water : Insoluble

Ethanol : Insoluble

몰농도 계산기

질량 농도 부피 분자량
희석 계산기 분자량 계산기

In vivo
배치:

생체 내 제형 계산기 (투명한 용액)

1단계: 아래 정보 입력 (권장: 실험 중 손실을 고려하여 추가 동물 포함)

mg/kg g μL

2단계: 생체 내 제형 입력 (이것은 계산기일 뿐 제형이 아닙니다. 용해도 섹션에 생체 내 제형이 없는 경우 먼저 당사에 문의하십시오.)

% DMSO % % Tween 80 % ddH2O
%DMSO %

계산 결과:

작업 농도: mg/ml;

DMSO 원액 준비 방법: mg 약물 사전 용해 μL DMSO ( 원액 농도 mg/mL, 농도가 해당 약물 배치의 DMSO 용해도를 초과하는 경우 먼저 당사에 문의하십시오. )

생체 내 제형 준비 방법: 취하다 μL DMSO 원액, 다음 추가μL PEG300, 혼합하고 투명하게 한 다음 추가μL Tween 80, 혼합하고 투명하게 한 다음 추가 μL ddH2O, 혼합하고 투명하게 합니다.

생체 내 제형 준비 방법: 취하다 μL DMSO 원액, 다음 추가 μL 옥수수 기름, 혼합하고 투명하게 합니다.

참고: 1. 다음 용매를 추가하기 전에 액체가 투명한지 확인하십시오.
2. 용매를 순서대로 추가해야 합니다. 다음 용매를 추가하기 전에 이전 추가에서 얻은 용액이 투명한 용액인지 확인해야 합니다. 와동, 초음파 또는 뜨거운 물 중탕과 같은 물리적 방법을 사용하여 용해를 도울 수 있습니다.

작용 메커니즘 (Mechanism of Action)

Targets/IC50/Ki
Raf-1
(Cell-free assay)
6 nM
mVEGFR2(Flk1)
(Cell-free assay)
15 nM
mVEGFR3
(Cell-free assay)
20 nM
B-Raf
(Cell-free assay)
22 nM
B-Raf (V599E)
(Cell-free assay)
38 nM
mPDGFRβ
(Cell-free assay)
57 nM
FLT3
(Cell-free assay)
58 nM
c-Kit
(Cell-free assay)
68 nM
VEGFR2
(Cell-free assay)
90 nM
FGFR1
(Cell-free assay)
580 nM
시험관 내(In vitro)
Sorafenib inhibits both wild-type and V599E mutant B-Raf activity with IC50 of 22 nM and 38 nM, respectively. This compound also potently inhibits mVEGFR2 (Flk-1), mVEGFR3, mPDGFRβ, Flt3, and c-Kit with IC50 of 15 nM, 20 nM, 57 nM, 58 nM, and 68 nM, respectively. It weakly inhibits FGFR-1 with IC50 of 580 nM. This chemical is not active against ERK-1, MEK-1, EGFR, HER-2, IGFR-1, c-Met, PKB, PKA, cdk1/cyclinB, PKCα, PKCγ, and pim-1. It markedly inhibits VEGFR2 phosphorylation in NIH 3T3 cells with IC50 of 30 nM, and Flt-3 phosphorylation in HEK-293 cells with IC50 of 20 nM. This agent potently blocks MEK 1/2 and ERK 1/2 phosphorylation in most cell lines but not in A549 or H460 cells, while having no effect on inhibition of the PKB pathway. It inhibits the proliferation of HAoSMC and MDA-MB-231 cells with IC50 of 0.28 μM and 2.6 μM, respectively. In addition to inhibition of the RAF/MEK/ERK signaling pathway, this compound significantly inhibits the phosphorylation of eIF4E and down-regulates Mcl-1 levels in hepatocellular carcinoma (HCC) cells in a MEK/ERK-independent manner. It inhibits the proliferation of PLC/PRF/5 and HepG2 cells with IC50 of 6.3 μM and 4.5 μM, respectively, and leads to the significant induction of apoptosis.
키나아제 분석
Biochemical assays
Recombinant baculoviruses expressing Raf-1 (residues 305–648) and B-Raf (residues 409–765) are purified as fusion proteins. Full-length human MEK-1 is generated by PCR and purified as a fusion protein from Escherichia coli lysates. Sorafenib tosylate is added to a mixture of Raf-1 (80 ng), or B-Raf (80 ng) with MEK-1 (1 μg) in assay buffer [20 mM Tris (pH 8.2), 100 mM NaCl, 5 mM MgCl2, and 0.15% β-mercaptoethanol] at a final concentration of 1% DMSO. The Raf kinase assay (final volume of 50 μL) is initiated by adding 25 μL of 10 μM γ[33P]ATP (400 Ci/mol) and incubated at 32 °C for 25 minutes. Phosphorylated MEK-1 is harvested by filtration onto a phosphocellulose mat, and 1% phosphoric acid is used to wash away unbound radioactivity. After drying by microwave heating, a β-plate counter is used to quantify filter-bound radioactivity. Human VEGFR2 (KDR) kinase domain is expressed and purified from Sf9 lysates. Time-resolved fluorescence energy transfer assays for VEGFR2 are performed in 96-well opaque plates in the time-resolved fluorescence energy transfer format. Final reaction conditions are as follows: 1 to 10 μM ATP, 25 nM poly GT-biotin, 2 nM Europium-labeled phospho (p)-Tyr antibody (PY20), 10 nM APC, 1 to 7 nM cytoplasmic kinase domain in final concentrations of 1% DMSO, 50 mM HEPES (pH 7.5), 10 mM MgCl2, 0.1 mM EDTA, 0.015% Brij-35, 0.1 mg/mL BSA, and 0.1% β-mercaptoethanol. Reaction volumes are 100 μL and are initiated by addition of enzyme. Plates are read at both 615 and 665 nM on a Perkin-Elmer VictorV Multilabel counter at ~1.5 to 2.0 hours after reaction initiation. Signal is calculated as a ratio: (665 nm/615 nM) × 10,000 for each well. For IC50 generation, this compound is added before the enzyme initiation. A 50-fold stock plate is made with this compound serially diluted 1:3 in a 50% DMSO/50% distilled water solution. Final concentrations of this chemical range from 10 μM to 4.56 nM in 1% DMSO.
생체 내(In vivo)
Oral administration of Sorafenib (~60 mg/kg) demonstrates broad spectrum, dose-dependent anti-tumor activity against a variety of human tumor xenograft models including MDA-MB-231, Colo-205, HT-29, DLD-1, NCI-H460, and A549, with no evidence of toxicity. In association with the anti-tumor efficacy, this compound treatment potently inhibits MEK 1/2 phosphorylation and pERK 1/2 levels in HT-29 and MDA-MB-231 xenografts but not in Colo-205 xenografts, and significantly suppresses tumor microvessel area (MVA) and microvessel density (MVD) in MDA MB-231, HT-29 and Colo-205 tumor xenografts. This agent produces dose-dependent growth inhibition of PLC/PRF/5 tumor xenografts in SCID mice with TGIs of 49% and 78% at 10 mg/kg and 30 mg/kg, respectively, consistent with the inhibition of ERK and eIF4E phosphorylation, reduction of the microvessel area, and induction of tumor cell apoptosis. It sensitizes bax-/- cells to TRAIL in a dose-dependent manner, through a mechanism involving down-regulating NF-κB mediated Mcl-1 and cIAP2 expression. Combining this compound (30-60 mg/kg) with TRAIL (5 mg/kg) show dramatic efficacy in TRAIL-resistant HCT116 bax-/- and HT29 tumor xenografts.
참조

적용 분야 (Applications)

방법 바이오마커 이미지 PMID
Western blot LC3-I / LC-3II / ATG5 p-STAT3 / STAT3 / Mcl-1 β-catenin / Survivin / Mcl-1 / PTMA pERK / ERK p-PKM2(y105) / PMK2 / Caspase-9 RET(pY1016) / VEGFR2(pY1214) / MEK1(pT292) / ERK(pY204) Cyclin D1
S7397-WB1
23392173
Growth inhibition assay Cell viability
S7397-viability1
26039995
Immunofluorescence p65 cytochrome c
S7397-IF1
22286758
ELISA TGF-beta / CD206 Caspase-9 / Caspase-3
S7397-ELISA1
26158762

임상시험 정보 (Clinical Trial Information)

(데이터 출처 https://clinicaltrials.gov, 업데이트 날짜 2024-05-22)

NCT 번호 모집 조건 스폰서/협력자 시작일 단계
NCT05068752 Recruiting
Pancreas Cancer
HonorHealth Research Institute|Bayer|Genentech Inc.
 October 28 2021 Phase 2
NCT04763408 Active not recruiting
Carcinoma Hepatocellular
Eisai Inc.
 April 9 2021 --