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
CAS: 878739-06-1
产品质控
AZ 628相关产品
相关信号通路图
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 |
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| 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] |
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|---|---|---|---|---|
| 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。 |
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| 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 |
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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) | |||
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体外溶解度 |
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 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
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
只
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，注：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：取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：取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
在订购、运输、储存和使用我们的产品的任何阶段，您遇到的任何问题，均可以通过拨打我们的热线电话400-668-6834，或者技术支持邮箱tech@selleck.cn，直接联系到我们。我们会在24小时内尽快联系您。
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