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Dasatinib Monohydrate Src 억제제

제품 번호S7782

Dasatinib Monohydrate (BMS-354825)는 Abl, Src 및 c-Kit을 표적으로 하는 새롭고 강력한 다중 표적 억제제로, 각각 <1 nM, 0.8 nM 및 79 nM의 IC50을 가집니다.
Dasatinib Monohydrate Src 억제제 Chemical Structure

화학 구조

분자량: 506.02

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품질 관리

배치: 순도: 99.62%
99.62

세포 배양, 처리 및 작업 농도

세포주 분석 유형 농도 배양 시간 제형 활성 설명 PMID
K562 cell Proliferation assay 72 h Antiproliferative activity against human K562 cells after 72 hrs, IC50=0.001 μM
WiDr cell Proliferation assay 72 h Antiproliferative activity against human WiDr cells after 72 hrs, IC50=0.052 μM
PC3 cell Proliferation assay 72 h Antiproliferative activity against human PC3 cells after 72 hrs, IC50=0.0094 μM
MDA-MB-231 cell Proliferation assay 72 h Antiproliferative activity against human MDA-MB-231 cells after 72 hrs, IC50=0.012 μM
M07ep210 cell Growth inhibition assay 48 h Growth inhibition of human M07ep210 cells after 48 hrs by [3H]thymidine uptake assay, IC50=0.07 nM
K562 cell Growth inhibition assay 48 h Growth inhibition of human K562 cells after 48 hrs by [3H]thymidine uptake assay, IC50=0.001 μM
M07e cell Growth inhibition assay 48 h Growth inhibition of human M07e cells after 48 hrs by [3H]thymidine uptake assay, IC50=0.0012 μM
K562 cell Cytotoxicity assay 72 h Cytotoxicity against human K562 cells after 72 hrs by WST-8 reagent based MTT assay, IC50=12.83 μM
U937 cell Cytotoxicity assay 72 h Cytotoxicity against human U937 cells after 72 hrs by WST-8 reagent based MTT assay, IC50=13.63 μM
K562 cell Proliferation assay 72 h Antiproliferative activity against human K562 cells after 72 hrs by CCK8 assay, IC50=0.7 nM
MDA-MB-435S cell Proliferation assay 72 h Antiproliferative activity against human MDA-MB-435S cells after 72 hrs by MTT assay, IC50=3.9 μM
NCI-H460 cell Proliferation assay 72 h Antiproliferative activity against human NCI-H460 cells after 72 hrs by MTT assay, IC50=8.99 μM
NCI-H23 cell Proliferation assay 72 h Antiproliferative activity against human NCI-H23 cells after 72 hrs by MTT assay, IC50=2.27 μM
A549 cell Proliferation assay 72 h Antiproliferative activity against human A549 cells after 72 hrs by MTT assay, IC50=12.66 μM
T47D cell Proliferation assay 72 h Antiproliferative activity against human T47D cells after 72 hrs by MTT assay, IC50=0.9 μM
HCT116 cell Proliferation assay 72 h Antiproliferative activity against human HCT116 cells after 72 hrs by MTT assay, IC50=2.3 μM
MCF7 cells Proliferation assay 72 h Antiproliferative activity against human MCF7 cells after 72 hrs by MTT assay, IC50=2.57 μM
RXF 393NL cell Cytotoxicity assay 4 days Cytotoxicity against human RXF 393NL cells after 4 days by propidium iodide staining, IC50=21.7 nM
PRXF DU145 cell Cytotoxicity assay 4 days Cytotoxicity against human PRXF DU145 cells after 4 days by propidium iodide staining, IC50=0.0623 μM
LXFA 983L cell Cytotoxicity assay 4 days Cytotoxicity against human LXFA 983L cells after 4 days by propidium iodide staining, IC50=56.5 nM
GXF251L cell Cytotoxicity assay 4 days Cytotoxicity against human GXF251L cells after 4 days by propidium iodide staining, IC50=2.25 μM
CXF 1103L cell Cytotoxicity assay 4 days Cytotoxicity against human CXF 1103L cells after 4 days by propidium iodide staining, IC50=4.36 μM
PAXF 1657L cell Cytotoxicity assay 4 days Cytotoxicity against human PAXF 1657L cells after 4 days by propidium iodide staining, IC50=0.121 μM
NCI-H1648 cell Growth inhibition assay Inhibition of human NCI-H1648 cell growth in a cell viability assay, IC50=0.02011 μM
NCI-H1838 cell Growth inhibition assay Inhibition of human NCI-H1838 cell growth in a cell viability assay, IC50=1.30733 μM
NCI-H2126 cell Growth inhibition assay Inhibition of human NCI-H2126 cell growth in a cell viability assay, IC50=2.87552 μM
NCI-H2141 cell Growth inhibition assay Inhibition of human NCI-H2141 cell growth in a cell viability assay, IC50=24.7754 μM
NCI-H2107 cell Growth inhibition assay Inhibition of human NCI-H2107 cell growth in a cell viability assay, IC50=43.4847 μM
NCI-H747 cell Growth inhibition assay Inhibition of human NCI-H747 cell growth in a cell viability assay, IC50=0.08362 μM
NCI-H720 cell Growth inhibition assay Inhibition of human NCI-H720 cell growth in a cell viability assay, IC50=20.2733 μM
NKM-1 cell Growth inhibition assay Inhibition of human NKM-1 cell growth in a cell viability assay.IC50=1.30859 μM
NMC-G1 cell Growth inhibition assay Inhibition of human NMC-G1 cell growth in a cell viability assay.IC50=0.11606 μM
NTERA-S-cl-D1 cell Growth inhibition assay Inhibition of human NTERA-S-cl-D1 cell growth in a cell viability assay.IC50=0.12283 μM
OCI-AML2 cell Growth inhibition assay Inhibition of human OCI-AML2 cell growth in a cell viability assay.IC50=5.86154 μM
OCUB-M cell Growth inhibition assay Inhibition of human OCUB-M cell growth in a cell viability assay.IC50=1.04412 μM
OPM-2 cell Growth inhibition assay Inhibition of human OPM-2 cell growth in a cell viability assay.IC50=4.27685 μM
OS-RC-2 cell Growth inhibition assay Inhibition of human OS-RC-2 cell growth in a cell viability assay.IC50=0.0203 μM
ONS-76 cell Growth inhibition assay Inhibition of human ONS-76 cell growth in a cell viability assay.IC50=0.42951 μM
OVCAR-4 cell Growth inhibition assay Inhibition of human OVCAR-4 cell growth in a cell viability assay.IC50=0.37433 μM
NCI-H446 cell Growth inhibition assay Inhibition of human NCI-H446 cell growth in a cell viability assay.IC50=0.6276 μM
NCI-H510A cell Growth inhibition assay Inhibition of human NCI-H510A cell growth in a cell viability assay.IC50=19.3973 μM
PF-382 cell Growth inhibition assay Inhibition of human PF-382 cell growth in a cell viability assay.IC50=0.17678 μM
NCI-H64 cell Growth inhibition assay Inhibition of human NCI-H64 cell growth in a cell viability assay.IC50=29.6253 μM
PSN1 cell Growth inhibition assay Inhibition of human PSN1 cell growth in a cell viability assay.IC50=0.04474 μM
QIMR-WIL cell Growth inhibition assay Inhibition of human QIMR-WIL cell growth in a cell viability assay.IC50=0.70629 μM
RL95-2 cell Growth inhibition assay Inhibition of human RL95-2 cell growth in a cell viability assay.IC50=0.1038 μM
RCC10RGB cell Growth inhibition assay Inhibition of human RCC10RGB cell growth in a cell viability assay.IC50=0.4911 μM
RKO cell Growth inhibition assay Inhibition of human RKO cell growth in a cell viability assay.IC50=0.52966 μM
NCI-SNU-16 cell Growth inhibition assay Inhibition of human NCI-SNU-16 cell growth in a cell viability assay.IC50=8.56128 μM
RPMI-6666 cell Growth inhibition assay Inhibition of human RPMI-6666 cell growth in a cell viability assay.IC50=7.27067 μM
NEC8 cell Growth inhibition assay Inhibition of human NEC8 cell growth in a cell viability assay.IC50=44.336 μM
RS4-11 cell Growth inhibition assay Inhibition of human RS4-11 cell growth in a cell viability assay.IC50=7.65787 μM
RXF393 cell Growth inhibition assay Inhibition of human RXF393 cell growth in a cell viability assay.IC50=0.02357 μM
Raji cell Growth inhibition assay Inhibition of human Raji cell growth in a cell viability assay.IC50=13.7497 μM
NOS-1 cell Growth inhibition assay Inhibition of human NOS-1 cell growth in a cell viability assay.IC50=0.006129 μM
SBC-1 cell Growth inhibition assay Inhibition of human SBC-1 cell growth in a cell viability assay.IC50=1.57984 μM
SF126 cell Growth inhibition assay Inhibition of human SF126 cell growth in a cell viability assay.IC50=0.3541 μM
SF539 cell Growth inhibition assay Inhibition of human SF539 cell growth in a cell viability assay.IC50=13.8557 μM
SH-4 cell Growth inhibition assay Inhibition of human SH-4 cell growth in a cell viability assay.IC50=0.18413 μM
OMC-1 cell Growth inhibition assay Inhibition of human OMC-1 cell growth in a cell viability assay.IC50=27.1422 μM
SIG-M5 cell Growth inhibition assay Inhibition of human SIG-M5 cell growth in a cell viability assay.IC50=9.02493 μM
SJSA-1 cell Growth inhibition assay Inhibition of human SJSA-1 cell growth in a cell viability assay.IC50=8.72805 μM
SK-LMS-1 cell Growth inhibition assay Inhibition of human SK-LMS-1 cell growth in a cell viability assay.IC50=3.11886 μM
SK-NEP-1 cell Growth inhibition assay Inhibition of human SK-NEP-1 cell growth in a cell viability assay.IC50=8.89155 μM
SKM-1 cell Growth inhibition assay Inhibition of human SKM-1 cell growth in a cell viability assay.IC50=9.01734 μM
SK-PN-DW cell Growth inhibition assay Inhibition of human SK-PN-DW cell growth in a cell viability assay.IC50=36.1943 μM
SK-UT-1 cell Growth inhibition assay Inhibition of human SK-UT-1 cell growth in a cell viability assay.IC50=2.16693 μM
SNB75 cell Growth inhibition assay Inhibition of human SNB75 cell growth in a cell viability assay.IC50=0.04435 μM
REH cell Growth inhibition assay Inhibition of human REH cell growth in a cell viability assay.IC50=20.6357 μM
SNU-C2B cell Growth inhibition assay Inhibition of human SNU-C2B cell growth in a cell viability assay.IC50=1.30589 μM
RPMI-8866 cell Growth inhibition assay Inhibition of human RPMI-8866 cell growth in a cell viability assay.IC50=17.4455 μM
SW872 cell Growth inhibition assay Inhibition of human SW872 cell growth in a cell viability assay.IC50=0.04161 μM
SW962 cell Growth inhibition assay Inhibition of human SW962 cell growth in a cell viability assay.IC50=0.11292 μM
SF268 cell Growth inhibition assay Inhibition of human SF268 cell growth in a cell viability assay.IC50=0.17404 μM
TE-1 cell Growth inhibition assay Inhibition of human TE-1 cell growth in a cell viability assay.IC50=0.1054 μM
8-MG-BA cell Growth inhibition assay Inhibition of human 8-MG-BA cell growth in a cell viability assay.IC50=0.15458 μM
A101D cell Growth inhibition assay Inhibition of human A101D cell growth in a cell viability assay.IC50=1.03043 μM
A253 cell Growth inhibition assay Inhibition of human A253 cell growth in a cell viability assay.IC50=3.73246 μM
A3-KAW cell Growth inhibition assay Inhibition of human A3-KAW cell growth in a cell viability assay.IC50=0.98452 μM
A4-Fuk cell Growth inhibition assay Inhibition of human A4-Fuk cell growth in a cell viability assay.IC50=38.1009 μM
A388 cell Growth inhibition assay Inhibition of human A388 cell growth in a cell viability assay.IC50=0.05095 μM
ACN cell Growth inhibition assay Inhibition of human ACN cell growth in a cell viability assay.IC50=1.82252 μM
A704 cell Growth inhibition assay Inhibition of human A704 cell growth in a cell viability assay.IC50=0.01491 μM
ALL-PO cell Growth inhibition assay Inhibition of human ALL-PO cell growth in a cell viability assay.IC50=10.7938 μM
ARH-77 cell Growth inhibition assay Inhibition of human ARH-77 cell growth in a cell viability assay.IC50=3.46915 μM
SR cell Growth inhibition assay Inhibition of human SR cell growth in a cell viability assay.IC50=4.49954 μM
BB65-RCC cell Growth inhibition assay Inhibition of human BB65-RCC cell growth in a cell viability assay.IC50=0.08227 μM
BB49-HNC cell Growth inhibition assay Inhibition of human BB49-HNC cell growth in a cell viability assay.IC50=0.38599 μM
BC-1 cell Growth inhibition assay Inhibition of human BC-1 cell growth in a cell viability assay.IC50=28.651 μM
BC-3 cell Growth inhibition assay Inhibition of human BC-3 cell growth in a cell viability assay.IC50=12.1138 μM
BL-41 cell Growth inhibition assay Inhibition of human BL-41 cell growth in a cell viability assay.IC50=0.29123 μM
BL-70 cell Growth inhibition assay Inhibition of human BL-70 cell growth in a cell viability assay.IC50=0.0000008218 μM
SW684 cell Growth inhibition assay Inhibition of human SW684 cell growth in a cell viability assay.IC50=0.3498 μM
BOKU cell Growth inhibition assay Inhibition of human BOKU cell growth in a cell viability assay.IC50=0.49133 μM
SW954 cell Growth inhibition assay Inhibition of human SW954 cell growth in a cell viability assay.IC50=0.02927 μM
C2BBe1 cell Growth inhibition assay Inhibition of human C2BBe1 cell growth in a cell viability assay.IC50=0.08308 μM
BV-173 cell Growth inhibition assay Inhibition of human BV-173 cell growth in a cell viability assay.IC50=0.000000109 μM
Becker cell Growth inhibition assay Inhibition of human Becker cell growth in a cell viability assay.IC50=0.03003 μM
SW982 cell Growth inhibition assay Inhibition of human SW982 cell growth in a cell viability assay.IC50=0.01115 μM
697 cell Growth inhibition assay Inhibition of human 697 cell growth in a cell viability assay.IC50=0.19987 μM
TE-15 cell Growth inhibition assay Inhibition of human TE-15 cell growth in a cell viability assay.IC50=0.005891 μM
TE-11 cell Growth inhibition assay Inhibition of human TE-11 cell growth in a cell viability assay.IC50=0.07858 μM
TE-5 cell Growth inhibition assay Inhibition of human TE-5 cell growth in a cell viability assay.IC50=1.79139 μM
TE-6 cell Growth inhibition assay Inhibition of human TE-6 cell growth in a cell viability assay.IC50=1.21226 μM
TE-9 cell Growth inhibition assay Inhibition of human TE-9 cell growth in a cell viability assay.IC50=0.87532 μM
TGBC24TKB cell Growth inhibition assay Inhibition of human TGBC24TKB cell growth in a cell viability assay.IC50=0.04761 μM
TGW cell Growth inhibition assay Inhibition of human TGW cell growth in a cell viability assay.IC50=11.2828 μM
TK10 cell Growth inhibition assay Inhibition of human TK10 cell growth in a cell viability assay.IC50=0.01174 μM
TGBC1TKB cell Growth inhibition assay Inhibition of human TGBC1TKB cell growth in a cell viability assay.IC50=0.06164 μM
A498 cell Growth inhibition assay Inhibition of human A498 cell growth in a cell viability assay.IC50=0.07284 μM
UACC-257 cell Growth inhibition assay Inhibition of human UACC-257 cell growth in a cell viability assay.IC50=12.9198 μM
U-87-MG cell Growth inhibition assay Inhibition of human U-87-MG cell growth in a cell viability assay.IC50=30.766 μM
BB30-HNC cell Growth inhibition assay Inhibition of human BB30-HNC cell growth in a cell viability assay.IC50=0.05437 μM
no-10 cell Growth inhibition assay Inhibition of human no-10 cell growth in a cell viability assay.IC50=0.31931 μM
CAS-1 cell Growth inhibition assay Inhibition of human CAS-1 cell growth in a cell viability assay.IC50=1.40992 μM
CGTH-W-1 cell Growth inhibition assay Inhibition of human CGTH-W-1 cell growth in a cell viability assay.IC50=0.03548 μM
TE-10 cell Growth inhibition assay Inhibition of human TE-10 cell growth in a cell viability assay.IC50=0.06357 μM
COLO-684 cell Growth inhibition assay Inhibition of human COLO-684 cell growth in a cell viability assay.IC50=46.2258 μM
TE-12 cell Growth inhibition assay Inhibition of human TE-12 cell growth in a cell viability assay.IC50=0.01861 μM
COR-L279 cell Growth inhibition assay Inhibition of human COR-L279 cell growth in a cell viability assay.IC50=40.2852 μM
TE-8 cell Growth inhibition assay Inhibition of human TE-8 cell growth in a cell viability assay.IC50=0.01576 μM
CP66-MEL cell Growth inhibition assay Inhibition of human CP66-MEL cell growth in a cell viability assay.IC50=0.19531 μM
CTV-1 cell Growth inhibition assay Inhibition of human CTV-1 cell growth in a cell viability assay.IC50=0.00004036 μM
VA-ES-BJ cell Growth inhibition assay Inhibition of human VA-ES-BJ cell growth in a cell viability assay.IC50=0.03902 μM
D-263MG cell Growth inhibition assay Inhibition of human D-263MG cell growth in a cell viability assay.IC50=0.36224 μM
D-336MG cell Growth inhibition assay Inhibition of human D-336MG cell growth in a cell viability assay.IC50=0.006298 μM
D-502MG cell Growth inhibition assay Inhibition of human D-502MG cell growth in a cell viability assay.IC50=1.23376 μM
DJM-1 cell Growth inhibition assay Inhibition of human DJM-1 cell growth in a cell viability assay.IC50=6.48558 μM
no-11 cell Growth inhibition assay Inhibition of human no-11 cell growth in a cell viability assay.IC50=0.50228 μM
DMS-153 cell Growth inhibition assay Inhibition of human DMS-153 cell growth in a cell viability assay.IC50=14.0028 μM
DSH1 cell Growth inhibition assay Inhibition of human DSH1 cell growth in a cell viability assay.IC50=0.24001 μM
DU-4475 cell Growth inhibition assay Inhibition of human DU-4475 cell growth in a cell viability assay.IC50=8.21652 μM
EB-3 cell Growth inhibition assay Inhibition of human EB-3 cell growth in a cell viability assay.IC50=34.3118 μM
EHEB cell Growth inhibition assay Inhibition of human EHEB cell growth in a cell viability assay.IC50=10.0656 μM
COLO-829 cell Growth inhibition assay Inhibition of human COLO-829 cell growth in a cell viability assay.IC50=0.12213 μM
CP67-MEL cell Growth inhibition assay Inhibition of human CP67-MEL cell growth in a cell viability assay.IC50=0.20488 μM
ES8 cell Growth inhibition assay Inhibition of human ES8 cell growth in a cell viability assay.IC50=32.1252 μM
EVSA-T cell Growth inhibition assay Inhibition of human EVSA-T cell growth in a cell viability assay.IC50=9.27793 μM
ES4 cell Growth inhibition assay Inhibition of human ES4 cell growth in a cell viability assay.IC50=1.05145 μM
ETK-1 cell Growth inhibition assay Inhibition of human ETK-1 cell growth in a cell viability assay.IC50=0.02832 μM
ES6 cell Growth inhibition assay Inhibition of human ES6 cell growth in a cell viability assay.IC50=0.03193 μM
EW-24 cell Growth inhibition assay Inhibition of human EW-24 cell growth in a cell viability assay.IC50=0.78165 μM
EoL-1-cell cell Growth inhibition assay Inhibition of human EoL-1-cell cell growth in a cell viability assay.IC50=0.00001309 μM
Calu-6 cell Growth inhibition assay Inhibition of human Calu-6 cell growth in a cell viability assay.IC50=3.05741 μM
GAK cell Growth inhibition assay Inhibition of human GAK cell growth in a cell viability assay.IC50=31.2686 μM
D-247MG cell Growth inhibition assay Inhibition of human D-247MG cell growth in a cell viability assay.IC50=6.12519 μM
GB-1 cell Growth inhibition assay Inhibition of human GB-1 cell growth in a cell viability assay.IC50=0.02157 μM
GI-ME-N cell Growth inhibition assay Inhibition of human GI-ME-N cell growth in a cell viability assay.IC50=0.06118 μM
GCIY cell Growth inhibition assay Inhibition of human GCIY cell growth in a cell viability assay.IC50=0.09656 μM
GT3TKB cell Growth inhibition assay Inhibition of human GT3TKB cell growth in a cell viability assay.IC50=9.35546 μM
HC-1 cell Growth inhibition assay Inhibition of human HC-1 cell growth in a cell viability assay.IC50=24.5551 μM
HAL-01 cell Growth inhibition assay Inhibition of human HAL-01 cell growth in a cell viability assay.IC50=19.7543 μM
HCC1187 cell Growth inhibition assay Inhibition of human HCC1187 cell growth in a cell viability assay.IC50=35.8052 μM
DEL cell Growth inhibition assay Inhibition of human DEL cell growth in a cell viability assay.IC50=41.9086 μM
HCC1599 cell Growth inhibition assay Inhibition of human HCC1599 cell growth in a cell viability assay.IC50=32.3325 μM
DOHH-2 cell Growth inhibition assay Inhibition of human DOHH-2 cell growth in a cell viability assay.IC50=0.01719 μM
HCC2157 cell Growth inhibition assay Inhibition of human HCC2157 cell growth in a cell viability assay.IC50=37.9946 μM
HCE-4 cell Growth inhibition assay Inhibition of human HCE-4 cell growth in a cell viability assay.IC50=0.26439 μM
HCE-T cell Growth inhibition assay Inhibition of human HCE-T cell growth in a cell viability assay.IC50=1.56714 μM
HEL cell Growth inhibition assay Inhibition of human HEL cell growth in a cell viability assay.IC50=10.4776 μM
EM-2 cell Growth inhibition assay Inhibition of human EM-2 cell growth in a cell viability assay.IC50=0.000001078 μM
HT-144 cell Growth inhibition assay Inhibition of human HT-144 cell growth in a cell viability assay.IC50=0.53609 μM
EW-16 cell Growth inhibition assay Inhibition of human EW-16 cell growth in a cell viability assay.IC50=0.76178 μM
IA-LM cell Growth inhibition assay Inhibition of human IA-LM cell growth in a cell viability assay.IC50=12.4445 μM
IST-MEL1 cell Growth inhibition assay Inhibition of human IST-MEL1 cell growth in a cell viability assay.IC50=0.1345 μM
IST-MES1 cell Growth inhibition assay Inhibition of human IST-MES1 cell growth in a cell viability assay.IC50=0.08552 μM
GI-1 cell Growth inhibition assay Inhibition of human GI-1 cell growth in a cell viability assay.IC50=1.3622 μM
IST-SL2 cell Growth inhibition assay Inhibition of human IST-SL2 cell growth in a cell viability assay.IC50=0.50302 μM
JVM-2 cell Growth inhibition assay Inhibition of human JVM-2 cell growth in a cell viability assay.IC50=2.36284 μM
JVM-3 cell Growth inhibition assay Inhibition of human JVM-3 cell growth in a cell viability assay.IC50=37.2338 μM
KALS-1 cell Growth inhibition assay Inhibition of human KALS-1 cell growth in a cell viability assay.IC50=0.0949 μM
KARPAS-422 cell Growth inhibition assay Inhibition of human KARPAS-422 cell growth in a cell viability assay.IC50=0.33997 μM
JiyoyeP-2003 cell Growth inhibition assay Inhibition of human JiyoyeP-2003 cell growth in a cell viability assay.IC50=1.73466 μM
KARPAS-45 cell Growth inhibition assay Inhibition of human KARPAS-45 cell growth in a cell viability assay.IC50=7.51671 μM
KGN cell Growth inhibition assay Inhibition of human KGN cell growth in a cell viability assay.IC50=0.01942 μM
KLE cell Growth inhibition assay Inhibition of human KLE cell growth in a cell viability assay.IC50=0.11317 μM
KNS-42 cell Growth inhibition assay Inhibition of human KNS-42 cell growth in a cell viability assay.IC50=1.24412 μM
KNS-81-FD cell Growth inhibition assay Inhibition of human KNS-81-FD cell growth in a cell viability assay.IC50=23.146 μM
KP-N-YS cell Growth inhibition assay Inhibition of human KP-N-YS cell growth in a cell viability assay.IC50=12.9283 μM
HOP-62 cell Growth inhibition assay Inhibition of human HOP-62 cell growth in a cell viability assay.IC50=0.01834 μM
KURAMOCHI cell Growth inhibition assay Inhibition of human KURAMOCHI cell growth in a cell viability assay.IC50=0.03487 μM
HUTU-80 cell Growth inhibition assay Inhibition of human HUTU-80 cell growth in a cell viability assay.IC50=0.3142 μM
LAMA-84 cell Growth inhibition assay Inhibition of human LAMA-84 cell growth in a cell viability assay.IC50=0.000003207 μM
LB1047-RCC cell Growth inhibition assay Inhibition of human LB1047-RCC cell growth in a cell viability assay.IC50=0.009887 μM
LB2518-MEL cell Growth inhibition assay Inhibition of human LB2518-MEL cell growth in a cell viability assay.IC50=0.14162 μM
LB373-MEL-D cell Growth inhibition assay Inhibition of human LB373-MEL-D cell growth in a cell viability assay.IC50=0.82508 μM
LB771-HNC cell Growth inhibition assay Inhibition of human LB771-HNC cell growth in a cell viability assay.IC50=2.57551 μM
LB996-RCC cell Growth inhibition assay Inhibition of human LB996-RCC cell growth in a cell viability assay.IC50=0.009912 μM
LC-2-ad cell Growth inhibition assay Inhibition of human LC-2-ad cell growth in a cell viability assay.IC50=0.02586 μM
J-RT3-T3-5 cell Growth inhibition assay Inhibition of human J-RT3-T3-5 cell growth in a cell viability assay.IC50=8.96529 μM
LP-1 cell Growth inhibition assay Inhibition of human LP-1 cell growth in a cell viability assay.IC50=7.54782 μM
K-562 cell Growth inhibition assay Inhibition of human K-562 cell growth in a cell viability assay.IC50=0.0000002656 μM
LS-123 cell Growth inhibition assay Inhibition of human LS-123 cell growth in a cell viability assay.IC50=0.14064 μM
K5 cell Growth inhibition assay Inhibition of human K5 cell growth in a cell viability assay.IC50=0.16489 μM
LS-411N cell Growth inhibition assay Inhibition of human LS-411N cell growth in a cell viability assay.IC50=48.4748 μM
KG-1 cell Growth inhibition assay Inhibition of human KG-1 cell growth in a cell viability assay.IC50=4.60845 μM
KINGS-1 cell Growth inhibition assay Inhibition of human KINGS-1 cell growth in a cell viability assay.IC50=0.16666 μM
LXF-289 cell Growth inhibition assay Inhibition of human LXF-289 cell growth in a cell viability assay.IC50=0.03956 μM
MC116 cell Growth inhibition assay Inhibition of human MC116 cell growth in a cell viability assay.IC50=0.1141 μM
KS-1 cell Growth inhibition assay Inhibition of human KS-1 cell growth in a cell viability assay.IC50=0.0273 μM
KU812 cell Growth inhibition assay Inhibition of human KU812 cell growth in a cell viability assay.IC50=0.11883 μM
MEG-01 cell Growth inhibition assay Inhibition of human MEG-01 cell growth in a cell viability assay.IC50=0.000009805 μM
MFH-ino cell Growth inhibition assay Inhibition of human MFH-ino cell growth in a cell viability assay.IC50=0.04724 μM
L-540 cell Growth inhibition assay Inhibition of human L-540 cell growth in a cell viability assay.IC50=15.0671 μM
MHH-NB-11 cell Growth inhibition assay Inhibition of human MHH-NB-11 cell growth in a cell viability assay.IC50=43.0818 μM
MMAC-SF cell Growth inhibition assay Inhibition of human MMAC-SF cell growth in a cell viability assay.IC50=8.79307 μM
LB2241-RCC cell Growth inhibition assay Inhibition of human LB2241-RCC cell growth in a cell viability assay.IC50=9.02012 μM
LB831-BLC cell Growth inhibition assay Inhibition of human LB831-BLC cell growth in a cell viability assay.IC50=0.04609 μM
MOLT-16 cell Growth inhibition assay Inhibition of human MOLT-16 cell growth in a cell viability assay.IC50=29.6292 μM
LC-1F cell Growth inhibition assay Inhibition of human LC-1F cell growth in a cell viability assay.IC50=27.3245 μM
MOLT-4 cell Growth inhibition assay Inhibition of human MOLT-4 cell growth in a cell viability assay.IC50=26.6753 μM
MZ1-PC cell Growth inhibition assay Inhibition of human MZ1-PC cell growth in a cell viability assay.IC50=0.03119 μM
MONO-MAC-6 cell Growth inhibition assay Inhibition of human MONO-MAC-6 cell growth in a cell viability assay.IC50=8.27066 μM
MZ2-MEL cell Growth inhibition assay Inhibition of human MZ2-MEL cell growth in a cell viability assay.IC50=0.28537 μM
MPP-89 cell Growth inhibition assay Inhibition of human MPP-89 cell growth in a cell viability assay.IC50=0.04049 μM
MZ7-mel cell Growth inhibition assay Inhibition of human MZ7-mel cell growth in a cell viability assay.IC50=0.47911 μM
LOXIMVI cell Growth inhibition assay Inhibition of human LOXIMVI cell growth in a cell viability assay.IC50=0.31503 μM
NALM-6 cell Growth inhibition assay Inhibition of human NALM-6 cell growth in a cell viability assay.IC50=0.19295 μM
NB13 cell Growth inhibition assay Inhibition of human NB13 cell growth in a cell viability assay.IC50=19.4877 μM
NB5 cell Growth inhibition assay Inhibition of human NB5 cell growth in a cell viability assay.IC50=1.39827 μM
NB17 cell Growth inhibition assay Inhibition of human NB17 cell growth in a cell viability assay.IC50=3.63847 μM
NCCIT cell Growth inhibition assay Inhibition of human NCCIT cell growth in a cell viability assay.IC50=2.86616 μM
NB69 cell Growth inhibition assay Inhibition of human NB69 cell growth in a cell viability assay.IC50=0.14436 μM
NCI-H1304 cell Growth inhibition assay Inhibition of human NCI-H1304 cell growth in a cell viability assay.IC50=28.1628 μM
NCI-H1395 cell Growth inhibition assay Inhibition of human NCI-H1395 cell growth in a cell viability assay.IC50=42.0163 μM
MHH-PREB-1 cell Growth inhibition assay Inhibition of human MHH-PREB-1 cell growth in a cell viability assay.IC50=0.74469 μM
MLMA cell Growth inhibition assay Inhibition of human MLMA cell growth in a cell viability assay.IC50=0.14032 μM
MN-60 cell Growth inhibition assay Inhibition of human MN-60 cell growth in a cell viability assay.IC50=15.1979 μM
MV-4-11 cell Growth inhibition assay Inhibition of human MV-4-11 cell growth in a cell viability assay.IC50=4.36454 μM
NB6 cell Growth inhibition assay Inhibition of human NB6 cell growth in a cell viability assay.IC50=9.92259 μM
NCI-H1355 cell Growth inhibition assay Inhibition of human NCI-H1355 cell growth in a cell viability assay.IC50=0.11028 μM
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화학 정보, 보관 및 안정성

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C22H28ClN7O3S

보관 (수령일로부터)
CAS 번호 863127-77-9 SDF 다운로드 원액 보관

동의어 BMS-354825 Monohydrate Smiles CC1=C(C(=CC=C1)Cl)NC(=O)C2=CN=C(S2)NC3=CC(=NC(=N3)C)N4CCN(CC4)CCO.O

용해도

In vitro
배치:

DMSO : 100 mg/mL (197.62 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
Abl
(Cell-free assay)
0.6 nM
Src
(Cell-free assay)
0.8 nM
c-Kit (D816V)
(Cell-free assay)
37 nM
c-Kit (wt)
(Cell-free assay)
79 nM
시험관 내(In vitro)
Dasatinib은 T315I를 제외하고 야생형 Bcr-Abl 및 Bcr-Abl 변이체를 발현하는 Ba/F3 세포의 증식을 억제하는 데 이마티닙보다 더 효과적입니다. Dasatinib은 이마티닙에 비해 2로그(약 325배) 증가된 효능을 가집니다. Dasatinib은 좁은 범위 내에서 야생형 Abl 키나아제와 T315I를 제외한 모든 변이체를 강력하게 억제합니다. Dasatinib은 야생형 및 변이형 Abl 키나아제 도메인을 직접 표적하고 농도 의존적으로 자가인산화 및 기질 인산화를 억제합니다. Dasatinib은 야생형 Bcr-Abl을 발현하는 세포에 대해 이마티닙보다 325배 더 큰 효능을 보입니다. TgE 골수 세포의 콜로니 비율은 미처리 웰의 100%에서 Dasatinib 처리 웰의 4.12%로 감소합니다. Dasatinib 존재 시, WT 및 TgE 골수 세포가 형성하는 콜로니 비율의 차이는 통계적으로 유의미합니다. LMP2A의 발현은 B 림프구 생존 및 증식을 촉진할 수 있으며, 이는 Dasatinib을 통해 Lyn 및/또는 c-Abl 키나아제를 표적함으로써 억제될 수 있습니다. Dasatinib 치료는 Src 신호 전달을 억제하고 성장을 감소시키며 특정 갑상선암 세포 하위 집단에서 세포 주기 정지 및 세포 사멸을 유도합니다. Dasatinib의 증량 투여(0.019 μM에서 1.25 μM)로 3일간 치료하면 C643, TPC1, BCPAP 및 SW1736 세포주의 성장이 낮은 나노몰 농도에서 약 50% 억제되는 반면, K1 세포주의 성장을 억제하려면 더 높은 농도가 필요합니다. 10 nM 또는 50 nM Dasatinib으로 치료하면 BCPAP, SW1736 및 K1 세포 중에서 G1 개체군의 세포가 9-22% 증가하고, S기 세포 비율은 7-18% 감소합니다.
키나아제 분석
키나아제 자가인산화 분석
야생형 및 변이형 글루타티온 S-트랜스퍼라제(GST)-Abl 융합 단백질(c-Abl 아미노산 220-498)을 사용하는 키나아제 분석을 수행합니다. GST-Abl 융합 단백질은 사용 전 글루타티온-세파로스 비드에서 방출됩니다. ATP 농도는 5μM입니다. 키나아제 자가인산화 및 시험관 내 펩타이드 기질 인산화 분석에 사용하기 직전에 GST-Abl 키나아제 도메인 융합 단백질은 LAR 티로신 포스파타제로 처리됩니다. 30°C에서 1시간 배양 후, LAR 포스파타제는 바나듐산나트륨(1mM) 첨가로 불활성화됩니다. 미처리 GST-Abl 키나아제와 탈인산화된 GST-Abl 키나아제를 비교하는 면역블롯 분석은 티로신 잔기의 완전한(>95%) 탈인산화를 확인하기 위해 포스포티로신 특이 항체 4G10을 사용하여 일상적으로 수행되며, GST-Abl 키나아제의 동일한 로딩을 확인하기 위해 c-Abl 항체 CST 2862를 사용합니다. Dasatinib 농도 범위는 변이체 T315I의 경우 1,000nM까지 확장됩니다. 이 동일한 억제제 농도는 시험관 내 펩타이드 기질 인산화 분석에 사용됩니다. 세 가지 억제제는 GST-Src 키나아제 및 GST-Lyn 키나아제에 대해 동일한 농도 범위에서 테스트됩니다.
생체 내(In vivo)
Dasatinib은 LMP2A/MYC 이중 형질전환 마우스의 비장 비대를 역전시킵니다. Dasatinib은 LMP2A를 발현하는 골수 B 세포의 콜로니 형성을 특이적으로 방지하고 TgE 마우스의 비장 크기를 감소시켰습니다. Dasatinib으로 처리한 Tg6/λ-MYC 마우스의 비장 질량은 대조군과 비교하여 유의하게 감소했습니다. Dasatinib은 LMP2A/MYC 이중 형질전환 마우스의 림프절 비대를 억제합니다. Dasatinib은 LMP2A/MYC 이중 형질전환 마우스의 종양 세포를 이식한 Rag1KO 마우스의 비장 비대를 역전시킵니다. Dasatinib 요법은 LMP2A를 발현하는 B 림프구 종양에서 Lyn 인산화를 억제합니다.
참조
  • [4] https://pubmed.ncbi.nlm.nih.gov/22586301/

적용 분야

방법 바이오마커 이미지 PMID
Western blot phospho-c-Abl(Tyr245) / phospho-c-Src(Tyr416) p27 / p21 cleaved caspase 3 p-FAK/p-STAT3
S7782-WB1
23049975
Growth inhibition assay Cell viability
S7782-viability1
23721490
Immunofluorescence SRC / Met α-tubulin F-actin / Actinin-4 / Paxillin
S7782-IF1
26517812
ELISA TNF-α E-selectin VCAM-1
S7782-ELISA1
17684099

임상시험 정보

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

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자주 묻는 질문

질문 1:
What's the difference between S1021 and S7782?

답변:
Usually, hydrate will be more stable and dissolve better than free base. But this compound (S1021) dissolves better in DMSO than it (S7782).