AZ 628

AZ628 是一种新型泛Raf抑制剂,作用于BRAF,BRAFV600E和c-Raf-1,无细胞试验中IC50分别为105 nM,34 nM和29 nM,也抑制VEGFR2, DDR2, Lyn, Flt1, FMS等。AZ628 可诱导凋亡。

AZ 628 Chemical Structure

AZ 628 Chemical Structure

CAS: 878739-06-1

规格 价格 库存 购买数量
10mM (1mL in DMSO) RMB 2191.76 现货
5mg RMB 1225.39 现货
25mg RMB 3841.45 现货
更大包装 有超大折扣

400-668-6834

info@selleck.cn

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客户使用Selleck的AZ 628发表文献42

产品质控

批次: S274601 DMSO] 90 mg/mL] false] Water] Insoluble] false] Ethanol] Insoluble] false 纯度: 99.89%
99.89

AZ 628相关产品

相关信号通路图

Raf抑制剂选择性比较

细胞实验数据示例

细胞系 实验类型 给药浓度 孵育时间 活性描述 文献信息
LNCaP-FGC Antiproliferative assay 72 hrs Antiproliferative activity against human LNCaP-FGC cells expressing wild type BRAF after 72 hrs by MTS assay 23398453
NIH:OVCAR3 Antiproliferative assay 72 hrs Antiproliferative activity against human NIH:OVCAR3 cells expressing wild type BRAF after 72 hrs by MTS assay 23398453
MiaPaCa Antiproliferative assay 72 hrs Antiproliferative activity against human MiaPaCa cells expressing wild type BRAF after 72 hrs by MTS assay 23398453
A375 Function assay 75 mins Inhibition of BRAF V600E mutant in human A375 cells assessed as decrease in ERK phosphorylation after 75 mins by Western blotting analysis 23398453
A375 Antiproliferative assay 72 hrs Antiproliferative activity against human A375 cells expressing BRAF V600E mutant after 72 hrs by MTS assay 23398453
COLO205 Antiproliferative assay 72 hrs Antiproliferative activity against human COLO205 cells expressing BRAF V600E mutant after 72 hrs by MTS assay 23398453
MALME-3M Antiproliferative assay 72 hrs Antiproliferative activity against human MALME-3M cells expressing BRAF V600E mutant after 72 hrs by MTS assay 23398453
SK-MEL-3 Antiproliferative assay 72 hrs Antiproliferative activity against human SK-MEL-3 cells expressing BRAF V600E mutant after 72 hrs by MTS assay 23398453
SK-MEL-28 Antiproliferative assay 72 hrs Antiproliferative activity against human SK-MEL-28 cells expressing BRAF V600E mutant after 72 hrs by MTS assay 23398453
SK-MEL-24 Antiproliferative assay 72 hrs Antiproliferative activity against human SK-MEL-24 cells expressing BRAF V600E mutant after 72 hrs by MTS assay 23398453
DU145 Antiproliferative assay 72 hrs Antiproliferative activity against human DU145 cells expressing wild type BRAF after 72 hrs by MTS assay 23398453
A2058 Antiproliferative assay 72 hrs Antiproliferative activity against human A2058 cells expressing BRAF V600E mutant after 72 hrs by MTS assay 23398453
SW620 Antiproliferative assay 72 hrs Antiproliferative activity against human SW620 cells expressing wild type BRAF after 72 hrs by MTS assay 23398453
HT-29 Antiproliferative assay 72 hrs Antiproliferative activity against human HT-29 cells expressing BRAF V600E mutant after 72 hrs by MTS assay 23398453
A549 Antiproliferative assay 72 hrs Antiproliferative activity against human A549 cells expressing wild type BRAF after 72 hrs by MTS assay 23398453
MDA-MB-468 Antiproliferative assay 72 hrs Antiproliferative activity against human MDA-MB-468 cells expressing wild type BRAF after 72 hrs by MTS assay 23398453
HCT116 Antiproliferative assay 72 hrs Antiproliferative activity against human HCT116 cells expressing wild type BRAF after 72 hrs by MTS assay 23398453
MCF7 Antiproliferative assay 72 hrs Antiproliferative activity against human MCF7 cells expressing wild type BRAF after 72 hrs by MTS assay 23398453
SKBR3 Antiproliferative assay 72 hrs Antiproliferative activity against human SKBR3 cells expressing wild type BRAF after 72 hrs by MTS assay 23398453
MDA-MB-231 Antiproliferative assay 72 hrs Antiproliferative activity against human MDA-MB-231 cells expressing BRAF G464V mutant after 72 hrs by MTS assay 23398453
HCT15 Antiproliferative assay 72 hrs Antiproliferative activity against human HCT15 cells expressing wild type BRAF after 72 hrs by MTS assay 23398453
Calu6 Antiproliferative assay 72 hrs Antiproliferative activity against human Calu6 cells expressing wild type BRAF after 72 hrs by MTS assay 23398453
NCI-H460 Antiproliferative assay 72 hrs Antiproliferative activity against human NCI-H460 cells expressing wild type BRAF after 72 hrs by MTS assay 23398453
NCI-H23 Antiproliferative assay 72 hrs Antiproliferative activity against human NCI-H23 cells expressing wild type BRAF after 72 hrs by MTS assay 23398453
PANC1 Antiproliferative assay 72 hrs Antiproliferative activity against human PANC1 cells expressing wild type BRAF after 72 hrs by MTS assay 23398453
PC3 Antiproliferative assay 72 hrs Antiproliferative activity against human PC3 cells expressing wild type BRAF after 72 hrs by MTS assay 23398453
A549 Function assay 75 mins Inhibition of wild type BRAF in human A549 cells assessed as decrease in ERK phosphorylation after 75 mins by Western blotting analysis 23398453
MCF7 Function assay 75 mins Inhibition of wild type BRAF in human MCF7 cells assessed as decrease in ERK phosphorylation after 75 mins by Western blotting analysis 23398453
CCD-1070SK Function assay 75 mins Inhibition of wild type BRAF in human CCD-1070SK cells assessed as decrease in ERK phosphorylation after 75 mins by Western blotting analysis 23398453
NIH/3T3 Function assay 75 mins Inhibition of wild type BRAF in mouse NIH/3T3 cells assessed as decrease in ERK phosphorylation after 75 mins by Western blotting analysis 23398453
Sf9 Function assay 20 mins Inhibition of human recombinant N-terminus His-tagged BRAF expressed in Sf9 cells coexpressing CDC37 using biotinylated MEK as substrate and MgCl2 incubated for 20 mins prior to MgCl2 addition measured after 1 hr in presence of 5 mM ATP, IC50=2.64μM 23398453
Sf9 Function assay 20 mins Inhibition of human recombinant N-terminus His-tagged BRAF V600E mutant expressed in Sf9 cells coexpressing CDC37 using biotinylated MEK as substrate and MgCl2 incubated for 20 mins prior to MgCl2 addition measured after 1 hr in presence of 5 mM ATP, IC50=0.27μM 23398453
Sf9 Function assay 20 mins Inhibition of human recombinant N-terminus His-tagged BRAF V600E mutant expressed in Sf9 cells coexpressing CDC37 using biotinylated MEK as substrate and MgCl2 incubated for 20 mins prior to MgCl2 addition measured after 1 hr in presence of 10 uM ATP, IC50=0.034μM 23398453
A375 Function assay 75 mins Inhibition of BRAF V600E mutant-mediated ERK phosphorylation in human A375 cells after 75 mins, IC50=0.015μM 23398453
A253 Growth inhibition assay Inhibition of human A253 cell growth in a cell viability assay, IC50=32.9626μM SANGER
BC-1 Growth inhibition assay Inhibition of human BC-1 cell growth in a cell viability assay, IC50=32.527μM SANGER
MOLT-16 Growth inhibition assay Inhibition of human MOLT-16 cell growth in a cell viability assay, IC50=32.0214μM SANGER
CTB-1 Growth inhibition assay Inhibition of human CTB-1 cell growth in a cell viability assay, IC50=31.889μM SANGER
IST-MES1 Growth inhibition assay Inhibition of human IST-MES1 cell growth in a cell viability assay, IC50=29.329μM SANGER
HCE-T Growth inhibition assay Inhibition of human HCE-T cell growth in a cell viability assay, IC50=29.2587μM SANGER
NCI-SNU-16 Growth inhibition assay Inhibition of human NCI-SNU-16 cell growth in a cell viability assay, IC50=27.7795μM SANGER
MHH-PREB-1 Growth inhibition assay Inhibition of human MHH-PREB-1 cell growth in a cell viability assay, IC50=27.9604μM SANGER
NCI-H2126 Growth inhibition assay Inhibition of human NCI-H2126 cell growth in a cell viability assay, IC50=27.6384μM SANGER
SK-PN-DW Growth inhibition assay Inhibition of human SK-PN-DW cell growth in a cell viability assay, IC50=27.3933μM SANGER
ES8 Growth inhibition assay Inhibition of human ES8 cell growth in a cell viability assay, IC50=26.1087μM SANGER
TE-8 Growth inhibition assay Inhibition of human TE-8 cell growth in a cell viability assay, IC50=26.0599μM SANGER
Ramos-2G6-4C10 Growth inhibition assay Inhibition of human Ramos-2G6-4C10 cell growth in a cell viability assay, IC50=26.0093μM SANGER
KNS-81-FD Growth inhibition assay Inhibition of human KNS-81-FD cell growth in a cell viability assay, IC50=25.8563μM SANGER
RL Growth inhibition assay Inhibition of human RL cell growth in a cell viability assay, IC50=25.1477μM SANGER
MC-CAR Growth inhibition assay Inhibition of human MC-CAR cell growth in a cell viability assay, IC50=25.0901μM SANGER
SF126 Growth inhibition assay Inhibition of human SF126 cell growth in a cell viability assay, IC50=24.9217μM SANGER
LS-1034 Growth inhibition assay Inhibition of human LS-1034 cell growth in a cell viability assay, IC50=24.2647μM SANGER
Raji Growth inhibition assay Inhibition of human Raji cell growth in a cell viability assay, IC50=23.4081μM SANGER
EKVX Growth inhibition assay Inhibition of human EKVX cell growth in a cell viability assay, IC50=23.7929μM SANGER
no-10 Growth inhibition assay Inhibition of human no-10 cell growth in a cell viability assay, IC50=22.5132μM SANGER
D-263MG Growth inhibition assay Inhibition of human D-263MG cell growth in a cell viability assay, IC50=22.9998μM SANGER
HCC2157 Growth inhibition assay Inhibition of human HCC2157 cell growth in a cell viability assay, IC50=22.2184μM SANGER
HH Growth inhibition assay Inhibition of human HH cell growth in a cell viability assay, IC50=21.8318μM SANGER
EB-3 Growth inhibition assay Inhibition of human EB-3 cell growth in a cell viability assay, IC50=21.8562μM SANGER
D-336MG Growth inhibition assay Inhibition of human D-336MG cell growth in a cell viability assay, IC50=33.9563μM SANGER
Becker Growth inhibition assay Inhibition of human Becker cell growth in a cell viability assay, IC50=21.5612μM SANGER
DSH1 Growth inhibition assay Inhibition of human DSH1 cell growth in a cell viability assay, IC50=21.3697μM SANGER
NALM-6 Growth inhibition assay Inhibition of human NALM-6 cell growth in a cell viability assay, IC50=21.2955μM SANGER
KURAMOCHI Growth inhibition assay Inhibition of human KURAMOCHI cell growth in a cell viability assay, IC50=20.7537μM SANGER
NCI-H1581 Growth inhibition assay Inhibition of human NCI-H1581 cell growth in a cell viability assay, IC50=20.5843μM SANGER
KARPAS-45 Growth inhibition assay Inhibition of human KARPAS-45 cell growth in a cell viability assay, IC50=20.4183μM SANGER
ES6 Growth inhibition assay Inhibition of human ES6 cell growth in a cell viability assay, IC50=20.3657μM SANGER
NCI-H64 Growth inhibition assay Inhibition of human NCI-H64 cell growth in a cell viability assay, IC50=19.9518μM SANGER
AM-38 Growth inhibition assay Inhibition of human AM-38 cell growth in a cell viability assay, IC50=19.7389μM SANGER
NCI-H128 Growth inhibition assay Inhibition of human NCI-H128 cell growth in a cell viability assay, IC50=19.2368μM SANGER
CRO-AP2 Growth inhibition assay Inhibition of human CRO-AP2 cell growth in a cell viability assay, IC50=18.6171μM SANGER
JVM-2 Growth inhibition assay Inhibition of human JVM-2 cell growth in a cell viability assay, IC50=18.6058μM SANGER
LU-65 Growth inhibition assay Inhibition of human LU-65 cell growth in a cell viability assay, IC50=18.5947μM SANGER
KY821 Growth inhibition assay Inhibition of human KY821 cell growth in a cell viability assay, IC50=18.4608μM SANGER
COLO-800 Growth inhibition assay Inhibition of human COLO-800 cell growth in a cell viability assay, IC50=18.0144μM SANGER
SF539 Growth inhibition assay Inhibition of human SF539 cell growth in a cell viability assay, IC50=17.8653μM SANGER
CAS-1 Growth inhibition assay Inhibition of human CAS-1 cell growth in a cell viability assay, IC50=17.7612μM SANGER
SW954 Growth inhibition assay Inhibition of human SW954 cell growth in a cell viability assay, IC50=17.7495μM SANGER
JiyoyeP-2003 Growth inhibition assay Inhibition of human JiyoyeP-2003 cell growth in a cell viability assay, IC50=17.2361μM SANGER
NCI-H716 Growth inhibition assay Inhibition of human NCI-H716 cell growth in a cell viability assay, IC50=16.9882μM SANGER
MONO-MAC-6 Growth inhibition assay Inhibition of human MONO-MAC-6 cell growth in a cell viability assay, IC50=16.6532μM SANGER
LOXIMVI Growth inhibition assay Inhibition of human LOXIMVI cell growth in a cell viability assay, IC50=16.4329μM SANGER
NTERA-S-cl-D1 Growth inhibition assay Inhibition of human NTERA-S-cl-D1 cell growth in a cell viability assay, IC50=16.395μM SANGER
TE-1 Growth inhibition assay Inhibition of human TE-1 cell growth in a cell viability assay, IC50=15.5684μM SANGER
CCRF-CEM Growth inhibition assay Inhibition of human CCRF-CEM cell growth in a cell viability assay, IC50=15.2306μM SANGER
LC4-1 Growth inhibition assay Inhibition of human LC4-1 cell growth in a cell viability assay, IC50=15.1355μM SANGER
NCI-H1355 Growth inhibition assay Inhibition of human NCI-H1355 cell growth in a cell viability assay, IC50=14.9946μM SANGER
HC-1 Growth inhibition assay Inhibition of human HC-1 cell growth in a cell viability assay, IC50=14.7737μM SANGER
NCI-H23 Growth inhibition assay Inhibition of human NCI-H23 cell growth in a cell viability assay, IC50=14.724μM SANGER
LP-1 Growth inhibition assay Inhibition of human LP-1 cell growth in a cell viability assay, IC50=14.4661μM SANGER
U-698-M Growth inhibition assay Inhibition of human U-698-M cell growth in a cell viability assay, IC50=14.435μM SANGER
GI-1 Growth inhibition assay Inhibition of human GI-1 cell growth in a cell viability assay, IC50=14.1988μM SANGER
KALS-1 Growth inhibition assay Inhibition of human KALS-1 cell growth in a cell viability assay, IC50=14.1325μM SANGER
ES5 Growth inhibition assay Inhibition of human ES5 cell growth in a cell viability assay, IC50=13.9428μM SANGER
MDA-MB-134-VI Growth inhibition assay Inhibition of human MDA-MB-134-VI cell growth in a cell viability assay, IC50=13.8879μM SANGER
SCLC-21H Growth inhibition assay Inhibition of human SCLC-21H cell growth in a cell viability assay, IC50=13.4345μM SANGER
NCI-H2171 Growth inhibition assay Inhibition of human NCI-H2171 cell growth in a cell viability assay, IC50=12.7506μM SANGER
SF268 Growth inhibition assay Inhibition of human SF268 cell growth in a cell viability assay, IC50=12.5572μM SANGER
EW-18 Growth inhibition assay Inhibition of human EW-18 cell growth in a cell viability assay, IC50=12.2119μM SANGER
RPMI-8402 Growth inhibition assay Inhibition of human RPMI-8402 cell growth in a cell viability assay, IC50=11.7395μM SANGER
LB2241-RCC Growth inhibition assay Inhibition of human LB2241-RCC cell growth in a cell viability assay, IC50=11.3688μM SANGER
GOTO Growth inhibition assay Inhibition of human GOTO cell growth in a cell viability assay, IC50=10.966μM SANGER
LS-123 Growth inhibition assay Inhibition of human LS-123 cell growth in a cell viability assay, IC50=10.5844μM SANGER
NB1 Growth inhibition assay Inhibition of human NB1 cell growth in a cell viability assay, IC50=10.5731μM SANGER
LB1047-RCC Growth inhibition assay Inhibition of human LB1047-RCC cell growth in a cell viability assay, IC50=10.5566μM SANGER
CA46 Growth inhibition assay Inhibition of human CA46 cell growth in a cell viability assay, IC50=10.5081μM SANGER
EoL-1-cell Growth inhibition assay Inhibition of human EoL-1-cell cell growth in a cell viability assay, IC50=9.93708μM SANGER
U-87-MG Growth inhibition assay Inhibition of human U-87-MG cell growth in a cell viability assay, IC50=9.78165μM SANGER
KE-37 Growth inhibition assay Inhibition of human KE-37 cell growth in a cell viability assay, IC50=9.49296μM SANGER
CESS Growth inhibition assay Inhibition of human CESS cell growth in a cell viability assay, IC50=9.3786μM SANGER
NCI-H322M Growth inhibition assay Inhibition of human NCI-H322M cell growth in a cell viability assay, IC50=9.28598μM SANGER
IM-9 Growth inhibition assay Inhibition of human IM-9 cell growth in a cell viability assay, IC50=9.06101μM SANGER
MFH-ino Growth inhibition assay Inhibition of human MFH-ino cell growth in a cell viability assay, IC50=8.9591μM SANGER
MLMA Growth inhibition assay Inhibition of human MLMA cell growth in a cell viability assay, IC50=8.65529μM SANGER
SK-UT-1 Growth inhibition assay Inhibition of human SK-UT-1 cell growth in a cell viability assay, IC50=8.59275μM SANGER
MOLT-4 Growth inhibition assay Inhibition of human MOLT-4 cell growth in a cell viability assay, IC50=8.51012μM SANGER
YT Growth inhibition assay Inhibition of human YT cell growth in a cell viability assay, IC50=8.11695μM SANGER
KU812 Growth inhibition assay Inhibition of human KU812 cell growth in a cell viability assay, IC50=8.02775μM SANGER
SR Growth inhibition assay Inhibition of human SR cell growth in a cell viability assay, IC50=7.64918μM SANGER
HAL-01 Growth inhibition assay Inhibition of human HAL-01 cell growth in a cell viability assay, IC50=7.45581μM SANGER
ECC4 Growth inhibition assay Inhibition of human ECC4 cell growth in a cell viability assay, IC50=7.2399μM SANGER
EHEB Growth inhibition assay Inhibition of human EHEB cell growth in a cell viability assay, IC50=7.13498μM SANGER
A388 Growth inhibition assay Inhibition of human A388 cell growth in a cell viability assay, IC50=6.70097μM SANGER
TK10 Growth inhibition assay Inhibition of human TK10 cell growth in a cell viability assay, IC50=6.64799μM SANGER
D-247MG Growth inhibition assay Inhibition of human D-247MG cell growth in a cell viability assay, IC50=6.63417μM SANGER
GB-1 Growth inhibition assay Inhibition of human GB-1 cell growth in a cell viability assay, IC50=6.57311μM SANGER
IST-SL2 Growth inhibition assay Inhibition of human IST-SL2 cell growth in a cell viability assay, IC50=6.51935μM SANGER
TE-9 Growth inhibition assay Inhibition of human TE-9 cell growth in a cell viability assay, IC50=6.42042μM SANGER
EB2 Growth inhibition assay Inhibition of human EB2 cell growth in a cell viability assay, IC50=6.33123μM SANGER
EW-11 Growth inhibition assay Inhibition of human EW-11 cell growth in a cell viability assay, IC50=6.27578μM SANGER
EW-22 Growth inhibition assay Inhibition of human EW-22 cell growth in a cell viability assay, IC50=6.09281μM SANGER
HOP-62 Growth inhibition assay Inhibition of human HOP-62 cell growth in a cell viability assay, IC50=6.06751μM SANGER
EW-3 Growth inhibition assay Inhibition of human EW-3 cell growth in a cell viability assay, IC50=5.87026μM SANGER
MOLT-13 Growth inhibition assay Inhibition of human MOLT-13 cell growth in a cell viability assay, IC50=5.82867μM SANGER
KGN Growth inhibition assay Inhibition of human KGN cell growth in a cell viability assay, IC50=5.69705μM SANGER
NEC8 Growth inhibition assay Inhibition of human NEC8 cell growth in a cell viability assay, IC50=5.68736μM SANGER
LC-2-ad Growth inhibition assay Inhibition of human LC-2-ad cell growth in a cell viability assay, IC50=5.66116μM SANGER
DJM-1 Growth inhibition assay Inhibition of human DJM-1 cell growth in a cell viability assay, IC50=5.63516μM SANGER
MPP-89 Growth inhibition assay Inhibition of human MPP-89 cell growth in a cell viability assay, IC50=5.53594μM SANGER
TE-5 Growth inhibition assay Inhibition of human TE-5 cell growth in a cell viability assay, IC50=5.39519μM SANGER
LB996-RCC Growth inhibition assay Inhibition of human LB996-RCC cell growth in a cell viability assay, IC50=5.28958μM SANGER
BC-3 Growth inhibition assay Inhibition of human BC-3 cell growth in a cell viability assay, IC50=5.25452μM SANGER
RPMI-6666 Growth inhibition assay Inhibition of human RPMI-6666 cell growth in a cell viability assay, IC50=5.08842μM SANGER
8-MG-BA Growth inhibition assay Inhibition of human 8-MG-BA cell growth in a cell viability assay, IC50=4.85156μM SANGER
HCC1599 Growth inhibition assay Inhibition of human HCC1599 cell growth in a cell viability assay, IC50=4.8017μM SANGER
NCI-H720 Growth inhibition assay Inhibition of human NCI-H720 cell growth in a cell viability assay, IC50=4.7198μM SANGER
SIMA Growth inhibition assay Inhibition of human SIMA cell growth in a cell viability assay, IC50=4.46019μM SANGER
EW-12 Growth inhibition assay Inhibition of human EW-12 cell growth in a cell viability assay, IC50=4.4199μM SANGER
SCC-15 Growth inhibition assay Inhibition of human SCC-15 cell growth in a cell viability assay, IC50=4.21476μM SANGER
KINGS-1 Growth inhibition assay Inhibition of human KINGS-1 cell growth in a cell viability assay, IC50=4.17422μM SANGER
RL95-2 Growth inhibition assay Inhibition of human RL95-2 cell growth in a cell viability assay, IC50=4.10119μM SANGER
HCC1187 Growth inhibition assay Inhibition of human HCC1187 cell growth in a cell viability assay, IC50=4.03307μM SANGER
L-540 Growth inhibition assay Inhibition of human L-540 cell growth in a cell viability assay, IC50=3.95889μM SANGER
MSTO-211H Growth inhibition assay Inhibition of human MSTO-211H cell growth in a cell viability assay, IC50=3.95028μM SANGER
KG-1 Growth inhibition assay Inhibition of human KG-1 cell growth in a cell viability assay, IC50=3.80547μM SANGER
SU-DHL-1 Growth inhibition assay Inhibition of human SU-DHL-1 cell growth in a cell viability assay, IC50=3.52915μM SANGER
LC-1F Growth inhibition assay Inhibition of human LC-1F cell growth in a cell viability assay, IC50=3.30326μM SANGER
QIMR-WIL Growth inhibition assay Inhibition of human QIMR-WIL cell growth in a cell viability assay, IC50=3.23473μM SANGER
SK-MEL-2 Growth inhibition assay Inhibition of human SK-MEL-2 cell growth in a cell viability assay, IC50=3.21751μM SANGER
PF-382 Growth inhibition assay Inhibition of human PF-382 cell growth in a cell viability assay, IC50=3.05237μM SANGER
OPM-2 Growth inhibition assay Inhibition of human OPM-2 cell growth in a cell viability assay, IC50=3.0342μM SANGER
HD-MY-Z Growth inhibition assay Inhibition of human HD-MY-Z cell growth in a cell viability assay, IC50=2.9442μM SANGER
BL-70 Growth inhibition assay Inhibition of human BL-70 cell growth in a cell viability assay, IC50=2.86352μM SANGER
NCI-SNU-5 Growth inhibition assay Inhibition of human NCI-SNU-5 cell growth in a cell viability assay, IC50=2.81269μM SANGER
TE-441-T Growth inhibition assay Inhibition of human TE-441-T cell growth in a cell viability assay, IC50=2.80668μM SANGER
EW-24 Growth inhibition assay Inhibition of human EW-24 cell growth in a cell viability assay, IC50=2.71195μM SANGER
RPMI-8226 Growth inhibition assay Inhibition of human RPMI-8226 cell growth in a cell viability assay, IC50=2.46647μM SANGER
D-502MG Growth inhibition assay Inhibition of human D-502MG cell growth in a cell viability assay, IC50=2.26142μM SANGER
KM12 Growth inhibition assay Inhibition of human KM12 cell growth in a cell viability assay, IC50=2.08103μM SANGER
DOHH-2 Growth inhibition assay Inhibition of human DOHH-2 cell growth in a cell viability assay, IC50=1.98728μM SANGER
BB30-HNC Growth inhibition assay Inhibition of human BB30-HNC cell growth in a cell viability assay, IC50=1.96472μM SANGER
NB5 Growth inhibition assay Inhibition of human NB5 cell growth in a cell viability assay, IC50=1.95406μM SANGER
SUP-T1 Growth inhibition assay Inhibition of human SUP-T1 cell growth in a cell viability assay, IC50=1.73943μM SANGER
ECC12 Growth inhibition assay Inhibition of human ECC12 cell growth in a cell viability assay, IC50=1.7149μM SANGER
LB373-MEL-D Growth inhibition assay Inhibition of human LB373-MEL-D cell growth in a cell viability assay, IC50=1.66482μM SANGER
SJSA-1 Growth inhibition assay Inhibition of human SJSA-1 cell growth in a cell viability assay, IC50=1.43007μM SANGER
MV-4-11 Growth inhibition assay Inhibition of human MV-4-11 cell growth in a cell viability assay, IC50=1.42334μM SANGER
ST486 Growth inhibition assay Inhibition of human ST486 cell growth in a cell viability assay, IC50=1.38662μM SANGER
ALL-PO Growth inhibition assay Inhibition of human ALL-PO cell growth in a cell viability assay, IC50=1.34869μM SANGER
TE-12 Growth inhibition assay Inhibition of human TE-12 cell growth in a cell viability assay, IC50=1.31417μM SANGER
GI-ME-N Growth inhibition assay Inhibition of human GI-ME-N cell growth in a cell viability assay, IC50=1.29212μM SANGER
NOMO-1 Growth inhibition assay Inhibition of human NOMO-1 cell growth in a cell viability assay, IC50=1.20638μM SANGER
CTV-1 Growth inhibition assay Inhibition of human CTV-1 cell growth in a cell viability assay, IC50=1.20065μM SANGER
HUTU-80 Growth inhibition assay Inhibition of human HUTU-80 cell growth in a cell viability assay, IC50=0.98331μM SANGER
BE-13 Growth inhibition assay Inhibition of human BE-13 cell growth in a cell viability assay, IC50=0.80575μM SANGER
MZ2-MEL Growth inhibition assay Inhibition of human MZ2-MEL cell growth in a cell viability assay, IC50=0.79367μM SANGER
NKM-1 Growth inhibition assay Inhibition of human NKM-1 cell growth in a cell viability assay, IC50=0.73537μM SANGER
BV-173 Growth inhibition assay Inhibition of human BV-173 cell growth in a cell viability assay, IC50=0.69154μM SANGER
LAN-6 Growth inhibition assay Inhibition of human LAN-6 cell growth in a cell viability assay, IC50=0.68236μM SANGER
NCI-H1648 Growth inhibition assay Inhibition of human NCI-H1648 cell growth in a cell viability assay, IC50=0.67266μM SANGER
K-562 Growth inhibition assay Inhibition of human K-562 cell growth in a cell viability assay, IC50=0.66695μM SANGER
NCI-H747 Growth inhibition assay Inhibition of human NCI-H747 cell growth in a cell viability assay, IC50=0.50637μM SANGER
NB14 Growth inhibition assay Inhibition of human NB14 cell growth in a cell viability assay, IC50=0.49331μM SANGER
A4-Fuk Growth inhibition assay Inhibition of human A4-Fuk cell growth in a cell viability assay, IC50=0.48375μM SANGER
SK-NEP-1 Growth inhibition assay Inhibition of human SK-NEP-1 cell growth in a cell viability assay, IC50=0.47226μM SANGER
NCI-SNU-1 Growth inhibition assay Inhibition of human NCI-SNU-1 cell growth in a cell viability assay, IC50=0.44786μM SANGER
KS-1 Growth inhibition assay Inhibition of human KS-1 cell growth in a cell viability assay, IC50=0.39337μM SANGER
SK-MEL-1 Growth inhibition assay Inhibition of human SK-MEL-1 cell growth in a cell viability assay, IC50=0.38362μM SANGER
MEG-01 Growth inhibition assay Inhibition of human MEG-01 cell growth in a cell viability assay, IC50=0.376μM SANGER
ML-2 Growth inhibition assay Inhibition of human ML-2 cell growth in a cell viability assay, IC50=0.36886μM SANGER
697 Growth inhibition assay Inhibition of human 697 cell growth in a cell viability assay, IC50=0.36388μM SANGER
D-392MG Growth inhibition assay Inhibition of human D-392MG cell growth in a cell viability assay, IC50=0.35607μM SANGER
BB49-HNC Growth inhibition assay Inhibition of human BB49-HNC cell growth in a cell viability assay, IC50=0.3518μM SANGER
MZ1-PC Growth inhibition assay Inhibition of human MZ1-PC cell growth in a cell viability assay, IC50=0.27999μM SANGER
GDM-1 Growth inhibition assay Inhibition of human GDM-1 cell growth in a cell viability assay, IC50=0.22947μM SANGER
HCC2998 Growth inhibition assay Inhibition of human HCC2998 cell growth in a cell viability assay, IC50=0.22187μM SANGER
IST-MEL1 Growth inhibition assay Inhibition of human IST-MEL1 cell growth in a cell viability assay, IC50=0.20413μM SANGER
EM-2 Growth inhibition assay Inhibition of human EM-2 cell growth in a cell viability assay, IC50=0.19591μM SANGER
LAMA-84 Growth inhibition assay Inhibition of human LAMA-84 cell growth in a cell viability assay, IC50=0.19242μM SANGER
NB69 Growth inhibition assay Inhibition of human NB69 cell growth in a cell viability assay, IC50=0.19131μM SANGER
ONS-76 Growth inhibition assay Inhibition of human ONS-76 cell growth in a cell viability assay, IC50=0.16662μM SANGER
HL-60 Growth inhibition assay Inhibition of human HL-60 cell growth in a cell viability assay, IC50=0.15441μM SANGER
K5 Growth inhibition assay Inhibition of human K5 cell growth in a cell viability assay, IC50=0.1342μM SANGER
CP66-MEL Growth inhibition assay Inhibition of human CP66-MEL cell growth in a cell viability assay, IC50=0.13176μM SANGER
CGTH-W-1 Growth inhibition assay Inhibition of human CGTH-W-1 cell growth in a cell viability assay, IC50=0.1213μM SANGER
MZ7-mel Growth inhibition assay Inhibition of human MZ7-mel cell growth in a cell viability assay, IC50=0.11727μM SANGER
KMOE-2 Growth inhibition assay Inhibition of human KMOE-2 cell growth in a cell viability assay, IC50=0.11588μM SANGER
SW872 Growth inhibition assay Inhibition of human SW872 cell growth in a cell viability assay, IC50=0.09648μM SANGER
NOS-1 Growth inhibition assay Inhibition of human NOS-1 cell growth in a cell viability assay, IC50=0.09265μM SANGER
LS-411N Growth inhibition assay Inhibition of human LS-411N cell growth in a cell viability assay, IC50=0.09161μM SANGER
LS-513 Growth inhibition assay Inhibition of human LS-513 cell growth in a cell viability assay, IC50=0.07415μM SANGER
Calu-6 Growth inhibition assay Inhibition of human Calu-6 cell growth in a cell viability assay, IC50=0.05147μM SANGER
MMAC-SF Growth inhibition assay Inhibition of human MMAC-SF cell growth in a cell viability assay, IC50=0.04007μM SANGER
RKO Growth inhibition assay Inhibition of human RKO cell growth in a cell viability assay, IC50=0.03767μM SANGER
UACC-257 Growth inhibition assay Inhibition of human UACC-257 cell growth in a cell viability assay, IC50=0.02749μM SANGER
PSN1 Growth inhibition assay Inhibition of human PSN1 cell growth in a cell viability assay, IC50=0.02737μM SANGER
COLO-829 Growth inhibition assay Inhibition of human COLO-829 cell growth in a cell viability assay, IC50=0.02565μM SANGER
OCI-AML2 Growth inhibition assay Inhibition of human OCI-AML2 cell growth in a cell viability assay, IC50=0.017μM SANGER
DU-4475 Growth inhibition assay Inhibition of human DU-4475 cell growth in a cell viability assay, IC50=0.01023μM SANGER
SIG-M5 Growth inhibition assay Inhibition of human SIG-M5 cell growth in a cell viability assay, IC50=0.009455μM SANGER
HT-144 Growth inhibition assay Inhibition of human HT-144 cell growth in a cell viability assay, IC50=0.006606μM SANGER
A101D Growth inhibition assay Inhibition of human A101D cell growth in a cell viability assay, IC50=0.005819μM SANGER
LB2518-MEL Growth inhibition assay Inhibition of human LB2518-MEL cell growth in a cell viability assay, IC50=0.004758μM SANGER
SH-4 Growth inhibition assay Inhibition of human SH-4 cell growth in a cell viability assay, IC50=0.003009μM SANGER
ACN Growth inhibition assay Inhibition of human ACN cell growth in a cell viability assay, IC50=0.0001009μM SANGER
RD qHTS assay qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for RD cells 29435139
NB1643 qHTS assay qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for NB1643 cells 29435139
SK-N-SH qHTS assay qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for SK-N-SH cells 29435139
NB-EBc1 qHTS assay qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for NB-EBc1 cells 29435139
SK-N-MC qHTS assay qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for SK-N-MC cells 29435139
A673 qHTS assay qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for A673 cells 29435139
Malme-3M Function assay Inhibition of B-Raf V600E mutant in human Malme-3M cells assessed as basal ERK phosphorylation, IC50=0.027μM 24675381
KARPAS-422 Growth inhibition assay Inhibition of human KARPAS-422 cell growth in a cell viability assay, IC50=34.5318μM SANGER
BB65-RCC Growth inhibition assay Inhibition of human BB65-RCC cell growth in a cell viability assay, IC50=36.0231μM SANGER
WSU-NHL Growth inhibition assay Inhibition of human WSU-NHL cell growth in a cell viability assay, IC50=36.1908μM SANGER
COLO-824 Growth inhibition assay Inhibition of human COLO-824 cell growth in a cell viability assay, IC50=37.3777μM SANGER
COR-L279 Growth inhibition assay Inhibition of human COR-L279 cell growth in a cell viability assay, IC50=37.3993μM SANGER
SK-N-FI Growth inhibition assay Inhibition of human SK-N-FI cell growth in a cell viability assay, IC50=38.3192μM SANGER
U-266 Growth inhibition assay Inhibition of human U-266 cell growth in a cell viability assay, IC50=38.8703μM SANGER
A3-KAW Growth inhibition assay Inhibition of human A3-KAW cell growth in a cell viability assay, IC50=39.1454μM SANGER
Daudi Growth inhibition assay Inhibition of human Daudi cell growth in a cell viability assay, IC50=42.5065μM SANGER
NCI-H1092 Growth inhibition assay Inhibition of human NCI-H1092 cell growth in a cell viability assay, IC50=43.345μM SANGER
NB10 Growth inhibition assay Inhibition of human NB10 cell growth in a cell viability assay, IC50=43.945μM SANGER
LXF-289 Growth inhibition assay Inhibition of human LXF-289 cell growth in a cell viability assay, IC50=44.786μM SANGER
MHH-NB-11 Growth inhibition assay Inhibition of human MHH-NB-11 cell growth in a cell viability assay, IC50=45.1968μM SANGER
LOUCY Growth inhibition assay Inhibition of human LOUCY cell growth in a cell viability assay, IC50=45.9997μM SANGER
DMS-114 Growth inhibition assay Inhibition of human DMS-114 cell growth in a cell viability assay, IC50=46.1196μM SANGER
NCI-H1882 Growth inhibition assay Inhibition of human NCI-H1882 cell growth in a cell viability assay, IC50=46.5042μM SANGER
ES3 Growth inhibition assay Inhibition of human ES3 cell growth in a cell viability assay, IC50=46.5616μM SANGER
OCUB-M Growth inhibition assay Inhibition of human OCUB-M cell growth in a cell viability assay, IC50=46.9249μM SANGER
TGW Growth inhibition assay Inhibition of human TGW cell growth in a cell viability assay, IC50=47.6222μM SANGER
OS-RC-2 Growth inhibition assay Inhibition of human OS-RC-2 cell growth in a cell viability assay, IC50=48.0389μM SANGER
D-542MG Growth inhibition assay Inhibition of human D-542MG cell growth in a cell viability assay, IC50=49.6469μM SANGER
点击查看更多细胞系数据

生物活性

产品描述 AZ628 是一种新型泛Raf抑制剂,作用于BRAF,BRAFV600E和c-Raf-1,无细胞试验中IC50分别为105 nM,34 nM和29 nM,也抑制VEGFR2, DDR2, Lyn, Flt1, FMS等。AZ628 可诱导凋亡。
靶点
C-Raf-1 [1]
(Cell-free assay)
B-Raf (V600E) [1]
(Cell-free assay)
B-Raf [1]
(Cell-free assay)
29 nM 34 nM 105 nM
体外研究(In Vitro)
体外研究活性 AZ628抑制B-Raf,B-RafV600E和c-Raf-1活性,IC50值分别为105,34和29 nM。AZ628也抑制多种酪氨酸蛋白激酶包括VEGFR2, DDR2, Lyn, Flt1, FMS等的激活。[1] AZ628作用于含B-RafV600E突变的结肠和恶性黑色素瘤细胞系,抑制锚蛋白依赖和非依赖性的生长, 引起细胞周期停滞,且诱导细胞凋亡。AZ628交叉反应谱说明AZ628和sorafenib相似,可以抗血管生成。[1] 用浓度不断升高的AZ628处理M14亲本细胞系,可观察到有效抑制p-ERK1/2水平。 抗AZ628的克隆表达CRAF提高。[2]提高的CRAF表达是抗连续AZ628处理的一种潜在机制,导致ERK1/2的持久激活。在对AZ628不敏感的细胞系中有三分之一用AZ628处理,不会明显抑制p-ERK1/2活性。AZ628作用于抗AZ628的M14细胞,不会抑制ERK的激活, AZ628作用于NRAS突变的恶性黑色素瘤细胞,有效降低ERK激活。[2]
细胞实验 细胞系 表达BRAFV600E突变的M14细胞
浓度 0.01-10 μM
孵育时间 过夜
方法 0.5-2.5×105个M14细胞接种在12或24孔板上,板上有含5% FBS的培养基。 温育过夜后细胞用不同浓度AZ628处理。每两天更换新鲜培养基和药物,直到对照组每孔融合一起。移除培养基,细胞和溶于PBS的4%甲醛在室温下混合20分钟。然后用PBS冲洗细胞两次,用1:5000荧光核酸染料Syto60溶液染色。使用Odyssey红外成像仪在700 nm处测量荧光信号密度。每组实验重复进行四次,结果为四次结果的平均值。
实验图片 检测方法 检测指标 实验图片 PMID
Western blot p-ERK / ERK / p-MEK / MEK / BIM / BRAF / CRAF 21098728
Growth inhibition assay Cell viability 21098728

化学信息&溶解度

分子量 451.52 分子式

C27H25N5O2

CAS号 878739-06-1 SDF Download AZ 628 SDF
Smiles CC1=C(C=C(C=C1)NC(=O)C2=CC(=CC=C2)C(C)(C)C#N)NC3=CC4=C(C=C3)N=CN(C4=O)C
储存条件(自收到货起)

体外溶解度
批次:

DMSO : 90 mg/mL ( 199.32 mM; DMSO吸湿会降低化合物溶解度,请使用新开封DMSO)

Water : Insoluble

Ethanol : Insoluble

摩尔浓度计算器

体内溶解度
批次:

现配现用,请按从左到右的顺序依次添加,澄清后再加入下一溶剂

动物体内配方计算器

实验计算

摩尔浓度计算器

质量 浓度 体积 分子量

动物体内配方计算器(澄清溶液)

第一步:请输入基本实验信息(考虑到实验过程中的损耗,建议多配一只动物的药量)

mg/kg g μL

第二步:请输入动物体内配方组成(配方适用于不溶于水的药物;不同批次药物配方比例不同,请联系Selleck为您提供正确的澄清溶液配方)

% DMSO % % Tween 80 % ddH2O
%DMSO %

计算结果:

工作液浓度: mg/ml;

DMSO母液配制方法: mg 药物溶于μL DMSO溶液(母液浓度mg/mL,:如该浓度超过该批次药物DMSO溶解度,请先联系Selleck);

体内配方配制方法:μL DMSO母液,加入μL PEG300,混匀澄清后加入μL Tween 80,混匀澄清后加入μL ddH2O,混匀澄清。

体内配方配制方法:μL DMSO母液,加入μL Corn oil,混匀澄清。

注意:1. 首先保证母液是澄清的;
2.一定要按照顺序依次将溶剂加入,进行下一步操作之前必须保证上一步操作得到的是澄清的溶液,可采用涡旋、超声或水浴加热等物理方法助溶。

技术支持

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