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Sorafenib (BAY 43-9006) Raf/VEGFR 억제제

제품 번호S7397

Sorafenib은 세포 없는 분석에서 각각 6 nM 및 22 nM의 IC50을 갖는 Raf-1B-Raf의 멀티키나아제 억제제입니다. Sorafenib은 VEGFR-2, VEGFR-3, PDGFR-β, Flt-3c-KIT를 각각 90 nM, 20 nM, 57 nM, 59 nM 및 68 nM의 IC50으로 억제합니다. Sorafenib은 AutophagyApoptosis를 유도하고 항암 활성과 함께 Ferroptosis를 활성화합니다.
Sorafenib (BAY 43-9006) Raf 억제제 Chemical Structure

화학 구조

분자량: 464.82

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품질 관리

배치: 순도: 99.91%
99.91

세포 배양, 처리 및 작업 농도

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

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

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

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)
Sorafenib은 야생형 및 V599E 돌연변이 B-Raf 활성을 각각 22 nM 및 38 nM의 IC50으로 억제합니다. 이 화합물은 또한 mVEGFR2 (Flk-1), mVEGFR3, mPDGFRβ, Flt3 및 c-Kit을 각각 15 nM, 20 nM, 57 nM, 58 nM 및 68 nM의 IC50으로 강력하게 억제합니다. FGFR-1을 580 nM의 IC50으로 약하게 억제합니다. 이 화학물질은 ERK-1, MEK-1, EGFR, HER-2, IGFR-1, c-Met, PKB, PKA, cdk1/cyclinB, PKCα, PKCγ 및 pim-1에 대해 활성이 없습니다. NIH 3T3 세포에서 VEGFR2 인산화를 30 nM의 IC50으로, HEK-293 세포에서 Flt-3 인산화를 20 nM의 IC50으로 현저하게 억제합니다. 이 약물은 대부분의 세포주에서 MEK 1/2 및 ERK 1/2 인산화를 강력하게 차단하지만 A549 또는 H460 세포에서는 그렇지 않으며, PKB 경로 억제에는 영향을 미치지 않습니다. HAoSMC 및 MDA-MB-231 세포의 증식을 각각 0.28 μM 및 2.6 μM의 IC50으로 억제합니다. RAF/MEK/ERK 신호 전달 경로 억제 외에도, 이 화합물은 MEK/ERK 독립적인 방식으로 간세포암종(HCC) 세포에서 eIF4E 인산화를 유의하게 억제하고 Mcl-1 수준을 하향 조절합니다. PLC/PRF/5 및 HepG2 세포의 증식을 각각 6.3 μM 및 4.5 μM의 IC50으로 억제하고, apoptosis의 유의한 유도를 유발합니다.
키나아제 분석
생화학 분석
Raf-1 (잔기 305–648) 및 B-Raf (잔기 409–765)를 발현하는 재조합 바큘로바이러스는 융합 단백질로 정제됩니다. 전장 인간 MEK-1은 PCR에 의해 생성되고 Escherichia coli 용해물에서 융합 단백질로 정제됩니다. Sorafenib 토실레이트는 분석 완충액 [20 mM Tris (pH 8.2), 100 mM NaCl, 5 mM MgCl2, 및 0.15% β-메르캅토에탄올] 내의 Raf-1 (80 ng) 또는 B-Raf (80 ng)와 MEK-1 (1 μg) 혼합물에 최종 농도 1% DMSO로 첨가됩니다. Raf 키나아제 분석 (최종 부피 50 μL)은 25 μL의 10 μM γ[33P]ATP (400 Ci/mol)를 첨가하여 시작되고 32 °C에서 25분 동안 배양됩니다. 인산화된 MEK-1은 포스포셀룰로스 매트 위에 여과하여 수확되고, 1% 인산이 비결합 방사능을 씻어내는 데 사용됩니다. 마이크로파 가열로 건조한 후, β-플레이트 카운터를 사용하여 필터에 결합된 방사능을 정량합니다. 인간 VEGFR2 (KDR) 키나아제 도메인은 Sf9 용해물에서 발현되고 정제됩니다. VEGFR2에 대한 시간 분해 형광 에너지 전달 분석은 시간 분해 형광 에너지 전달 형식의 96웰 불투명 플레이트에서 수행됩니다. 최종 반응 조건은 다음과 같습니다: 1 내지 10 μM ATP, 25 nM 폴리 GT-바이오틴, 2 nM 유로퓸 표지 인산화 (p)-Tyr 항체 (PY20), 10 nM APC, 1 내지 7 nM 세포질 키나아제 도메인 (최종 농도 1% DMSO, 50 mM HEPES (pH 7.5), 10 mM MgCl2, 0.1 mM EDTA, 0.015% Brij-35, 0.1 mg/mL BSA, 및 0.1% β-메르캅토에탄올). 반응 부피는 100 μL이며 효소 첨가로 시작됩니다. 플레이트는 반응 시작 후 약 1.5 내지 2.0시간에 Perkin-Elmer VictorV Multilabel 카운터에서 615 및 665 nM 모두에서 판독됩니다. 신호는 각 웰에 대해 비율: (665 nm/615 nM) × 10,000으로 계산됩니다. IC50 생성을 위해 이 화합물은 효소 시작 전에 첨가됩니다. 이 화합물을 50% DMSO/50% 증류수 용액에 1:3으로 연속 희석하여 50배 스톡 플레이트를 만듭니다. 이 화학물질의 최종 농도는 1% DMSO에서 10 μM 내지 4.56 nM입니다.
생체 내(In vivo)
Sorafenib (~60 mg/kg)의 경구 투여는 MDA-MB-231, Colo-205, HT-29, DLD-1, NCI-H460 및 A549를 포함한 다양한 인간 종양 이종이식 모델에 대해 광범위하고 용량 의존적인 항종양 활성을 나타내며 독성 증거는 없습니다. 항종양 효능과 관련하여, 이 화합물 치료는 HT-29 및 MDA-MB-231 이종이식편에서 MEK 1/2 인산화 및 pERK 1/2 수준을 강력하게 억제하지만 Colo-205 이종이식편에서는 억제하지 않으며, MDA MB-231, HT-29 및 Colo-205 종양 이종이식편에서 종양 미세혈관 면적 (MVA) 및 미세혈관 밀도 (MVD)를 유의하게 억제합니다. 이 약물은 SCID 마우스에서 PLC/PRF/5 종양 이종이식편의 용량 의존적 성장 억제를 유발하며, 10 mg/kg 및 30 mg/kg에서 각각 49% 및 78%의 TGI를 나타내어 ERK 및 eIF4E 인산화 억제, 미세혈관 면적 감소 및 종양 세포 apoptosis 유도와 일치합니다. NF-κB 매개 Mcl-1 및 cIAP2 발현 하향 조절을 포함하는 메커니즘을 통해 bax-/- 세포를 TRAIL에 용량 의존적으로 민감하게 만듭니다. 이 화합물 (30-60 mg/kg)과 TRAIL (5 mg/kg)을 병용하면 TRAIL 내성 HCT116 bax-/- 및 HT29 종양 이종이식편에서 극적인 효능을 보여줍니다.
참조

적용 분야

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

(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 --

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