Home MAPK Raf inhibitor - Apoptosis related activator AZ 628 For research use only.

AZ 628

AZ628 is a new pan-Raf inhibitor for BRAF, BRAFV600E, and c-Raf-1 with IC50 of 105 nM, 34 nM and 29 nM in cell-free assays, also inhibits VEGFR2, DDR2, Lyn, Flt1, FMS, etc. AZ628 induces apoptosis.

AZ 628 Chemical Structure

AZ 628 Chemical Structure

CAS No. 878739-06-1

Purity & Quality Control

Batch: S274601 DMSO]90 mg/mL]false]Water]Insoluble]false]Ethanol]Insoluble]false Purity: 99.89%
99.89

AZ 628 Related Products

Signaling Pathway

Raf Signaling Pathways

Raf Signaling Pathway

Cell Data

Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID
A375 Function assay 75 mins Inhibition of BRAF V600E mutant-mediated ERK phosphorylation in human A375 cells after 75 mins, IC50=0.015μM 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
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 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
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
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
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
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
PC3 Antiproliferative assay 72 hrs Antiproliferative activity against human PC3 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
NCI-H23 Antiproliferative assay 72 hrs Antiproliferative activity against human NCI-H23 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
Calu6 Antiproliferative assay 72 hrs Antiproliferative activity against human Calu6 cells expressing wild type BRAF 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
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
SKBR3 Antiproliferative assay 72 hrs Antiproliferative activity against human SKBR3 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
HCT116 Antiproliferative assay 72 hrs Antiproliferative activity against human HCT116 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
A549 Antiproliferative assay 72 hrs Antiproliferative activity against human A549 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
SW620 Antiproliferative assay 72 hrs Antiproliferative activity against human SW620 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
DU145 Antiproliferative assay 72 hrs Antiproliferative activity against human DU145 cells expressing wild type BRAF 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
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-3 Antiproliferative assay 72 hrs Antiproliferative activity against human SK-MEL-3 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
COLO205 Antiproliferative assay 72 hrs Antiproliferative activity against human COLO205 cells expressing BRAF V600E mutant after 72 hrs by MTS assay 23398453
A375 Antiproliferative assay 72 hrs Antiproliferative activity against human A375 cells expressing BRAF V600E mutant 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
MiaPaCa Antiproliferative assay 72 hrs Antiproliferative activity against human MiaPaCa 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
LNCaP-FGC Antiproliferative assay 72 hrs Antiproliferative activity against human LNCaP-FGC cells expressing wild type BRAF after 72 hrs by MTS assay 23398453
Malme-3M Function assay Inhibition of B-Raf V600E mutant in human Malme-3M cells assessed as basal ERK phosphorylation, IC50=0.027μM 24675381
A673 qHTS assay qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for A673 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
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-SH qHTS assay qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for SK-N-SH cells 29435139
NB1643 qHTS assay qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for NB1643 cells 29435139
RD qHTS assay qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for RD cells 29435139
ACN Growth inhibition assay Inhibition of human ACN cell growth in a cell viability assay, IC50=0.0001009μM SANGER
SH-4 Growth inhibition assay Inhibition of human SH-4 cell growth in a cell viability assay, IC50=0.003009μM SANGER
LB2518-MEL Growth inhibition assay Inhibition of human LB2518-MEL cell growth in a cell viability assay, IC50=0.004758μM SANGER
A101D Growth inhibition assay Inhibition of human A101D cell growth in a cell viability assay, IC50=0.005819μM SANGER
HT-144 Growth inhibition assay Inhibition of human HT-144 cell growth in a cell viability assay, IC50=0.006606μM SANGER
SIG-M5 Growth inhibition assay Inhibition of human SIG-M5 cell growth in a cell viability assay, IC50=0.009455μM SANGER
DU-4475 Growth inhibition assay Inhibition of human DU-4475 cell growth in a cell viability assay, IC50=0.01023μM SANGER
OCI-AML2 Growth inhibition assay Inhibition of human OCI-AML2 cell growth in a cell viability assay, IC50=0.017μM SANGER
COLO-829 Growth inhibition assay Inhibition of human COLO-829 cell growth in a cell viability assay, IC50=0.02565μM SANGER
PSN1 Growth inhibition assay Inhibition of human PSN1 cell growth in a cell viability assay, IC50=0.02737μM SANGER
UACC-257 Growth inhibition assay Inhibition of human UACC-257 cell growth in a cell viability assay, IC50=0.02749μM SANGER
RKO Growth inhibition assay Inhibition of human RKO cell growth in a cell viability assay, IC50=0.03767μM SANGER
MMAC-SF Growth inhibition assay Inhibition of human MMAC-SF cell growth in a cell viability assay, IC50=0.04007μM SANGER
Calu-6 Growth inhibition assay Inhibition of human Calu-6 cell growth in a cell viability assay, IC50=0.05147μM SANGER
LS-513 Growth inhibition assay Inhibition of human LS-513 cell growth in a cell viability assay, IC50=0.07415μM SANGER
LS-411N Growth inhibition assay Inhibition of human LS-411N cell growth in a cell viability assay, IC50=0.09161μM SANGER
NOS-1 Growth inhibition assay Inhibition of human NOS-1 cell growth in a cell viability assay, IC50=0.09265μM SANGER
SW872 Growth inhibition assay Inhibition of human SW872 cell growth in a cell viability assay, IC50=0.09648μM SANGER
KMOE-2 Growth inhibition assay Inhibition of human KMOE-2 cell growth in a cell viability assay, IC50=0.11588μM SANGER
MZ7-mel Growth inhibition assay Inhibition of human MZ7-mel cell growth in a cell viability assay, IC50=0.11727μM SANGER
CGTH-W-1 Growth inhibition assay Inhibition of human CGTH-W-1 cell growth in a cell viability assay, IC50=0.1213μM SANGER
CP66-MEL Growth inhibition assay Inhibition of human CP66-MEL cell growth in a cell viability assay, IC50=0.13176μM SANGER
K5 Growth inhibition assay Inhibition of human K5 cell growth in a cell viability assay, IC50=0.1342μM SANGER
HL-60 Growth inhibition assay Inhibition of human HL-60 cell growth in a cell viability assay, IC50=0.15441μM SANGER
ONS-76 Growth inhibition assay Inhibition of human ONS-76 cell growth in a cell viability assay, IC50=0.16662μM SANGER
NB69 Growth inhibition assay Inhibition of human NB69 cell growth in a cell viability assay, IC50=0.19131μM SANGER
LAMA-84 Growth inhibition assay Inhibition of human LAMA-84 cell growth in a cell viability assay, IC50=0.19242μM SANGER
EM-2 Growth inhibition assay Inhibition of human EM-2 cell growth in a cell viability assay, IC50=0.19591μM SANGER
IST-MEL1 Growth inhibition assay Inhibition of human IST-MEL1 cell growth in a cell viability assay, IC50=0.20413μM SANGER
HCC2998 Growth inhibition assay Inhibition of human HCC2998 cell growth in a cell viability assay, IC50=0.22187μM SANGER
GDM-1 Growth inhibition assay Inhibition of human GDM-1 cell growth in a cell viability assay, IC50=0.22947μM SANGER
MZ1-PC Growth inhibition assay Inhibition of human MZ1-PC cell growth in a cell viability assay, IC50=0.27999μM SANGER
BB49-HNC Growth inhibition assay Inhibition of human BB49-HNC cell growth in a cell viability assay, IC50=0.3518μM SANGER
D-392MG Growth inhibition assay Inhibition of human D-392MG cell growth in a cell viability assay, IC50=0.35607μM SANGER
697 Growth inhibition assay Inhibition of human 697 cell growth in a cell viability assay, IC50=0.36388μM SANGER
ML-2 Growth inhibition assay Inhibition of human ML-2 cell growth in a cell viability assay, IC50=0.36886μM SANGER
MEG-01 Growth inhibition assay Inhibition of human MEG-01 cell growth in a cell viability assay, IC50=0.376μM SANGER
SK-MEL-1 Growth inhibition assay Inhibition of human SK-MEL-1 cell growth in a cell viability assay, IC50=0.38362μM SANGER
KS-1 Growth inhibition assay Inhibition of human KS-1 cell growth in a cell viability assay, IC50=0.39337μM SANGER
NCI-SNU-1 Growth inhibition assay Inhibition of human NCI-SNU-1 cell growth in a cell viability assay, IC50=0.44786μM SANGER
SK-NEP-1 Growth inhibition assay Inhibition of human SK-NEP-1 cell growth in a cell viability assay, IC50=0.47226μM SANGER
A4-Fuk Growth inhibition assay Inhibition of human A4-Fuk cell growth in a cell viability assay, IC50=0.48375μM SANGER
NB14 Growth inhibition assay Inhibition of human NB14 cell growth in a cell viability assay, IC50=0.49331μM SANGER
NCI-H747 Growth inhibition assay Inhibition of human NCI-H747 cell growth in a cell viability assay, IC50=0.50637μM SANGER
K-562 Growth inhibition assay Inhibition of human K-562 cell growth in a cell viability assay, IC50=0.66695μM SANGER
NCI-H1648 Growth inhibition assay Inhibition of human NCI-H1648 cell growth in a cell viability assay, IC50=0.67266μM SANGER
LAN-6 Growth inhibition assay Inhibition of human LAN-6 cell growth in a cell viability assay, IC50=0.68236μM SANGER
BV-173 Growth inhibition assay Inhibition of human BV-173 cell growth in a cell viability assay, IC50=0.69154μM SANGER
NKM-1 Growth inhibition assay Inhibition of human NKM-1 cell growth in a cell viability assay, IC50=0.73537μM SANGER
MZ2-MEL Growth inhibition assay Inhibition of human MZ2-MEL cell growth in a cell viability assay, IC50=0.79367μM SANGER
BE-13 Growth inhibition assay Inhibition of human BE-13 cell growth in a cell viability assay, IC50=0.80575μM SANGER
HUTU-80 Growth inhibition assay Inhibition of human HUTU-80 cell growth in a cell viability assay, IC50=0.98331μM SANGER
CTV-1 Growth inhibition assay Inhibition of human CTV-1 cell growth in a cell viability assay, IC50=1.20065μM SANGER
NOMO-1 Growth inhibition assay Inhibition of human NOMO-1 cell growth in a cell viability assay, IC50=1.20638μM SANGER
GI-ME-N Growth inhibition assay Inhibition of human GI-ME-N cell growth in a cell viability assay, IC50=1.29212μM SANGER
TE-12 Growth inhibition assay Inhibition of human TE-12 cell growth in a cell viability assay, IC50=1.31417μM SANGER
ALL-PO Growth inhibition assay Inhibition of human ALL-PO cell growth in a cell viability assay, IC50=1.34869μM SANGER
ST486 Growth inhibition assay Inhibition of human ST486 cell growth in a cell viability assay, IC50=1.38662μM SANGER
MV-4-11 Growth inhibition assay Inhibition of human MV-4-11 cell growth in a cell viability assay, IC50=1.42334μM SANGER
SJSA-1 Growth inhibition assay Inhibition of human SJSA-1 cell growth in a cell viability assay, IC50=1.43007μM SANGER
LB373-MEL-D Growth inhibition assay Inhibition of human LB373-MEL-D cell growth in a cell viability assay, IC50=1.66482μM SANGER
ECC12 Growth inhibition assay Inhibition of human ECC12 cell growth in a cell viability assay, IC50=1.7149μM SANGER
SUP-T1 Growth inhibition assay Inhibition of human SUP-T1 cell growth in a cell viability assay, IC50=1.73943μM SANGER
NB5 Growth inhibition assay Inhibition of human NB5 cell growth in a cell viability assay, IC50=1.95406μM SANGER
BB30-HNC Growth inhibition assay Inhibition of human BB30-HNC cell growth in a cell viability assay, IC50=1.96472μM SANGER
DOHH-2 Growth inhibition assay Inhibition of human DOHH-2 cell growth in a cell viability assay, IC50=1.98728μM SANGER
KM12 Growth inhibition assay Inhibition of human KM12 cell growth in a cell viability assay, IC50=2.08103μM SANGER
D-502MG Growth inhibition assay Inhibition of human D-502MG cell growth in a cell viability assay, IC50=2.26142μM SANGER
RPMI-8226 Growth inhibition assay Inhibition of human RPMI-8226 cell growth in a cell viability assay, IC50=2.46647μM SANGER
EW-24 Growth inhibition assay Inhibition of human EW-24 cell growth in a cell viability assay, IC50=2.71195μM SANGER
TE-441-T Growth inhibition assay Inhibition of human TE-441-T cell growth in a cell viability assay, IC50=2.80668μM SANGER
NCI-SNU-5 Growth inhibition assay Inhibition of human NCI-SNU-5 cell growth in a cell viability assay, IC50=2.81269μM SANGER
BL-70 Growth inhibition assay Inhibition of human BL-70 cell growth in a cell viability assay, IC50=2.86352μM SANGER
HD-MY-Z Growth inhibition assay Inhibition of human HD-MY-Z cell growth in a cell viability assay, IC50=2.9442μM SANGER
OPM-2 Growth inhibition assay Inhibition of human OPM-2 cell growth in a cell viability assay, IC50=3.0342μM SANGER
PF-382 Growth inhibition assay Inhibition of human PF-382 cell growth in a cell viability assay, IC50=3.05237μM SANGER
SK-MEL-2 Growth inhibition assay Inhibition of human SK-MEL-2 cell growth in a cell viability assay, IC50=3.21751μM SANGER
QIMR-WIL Growth inhibition assay Inhibition of human QIMR-WIL cell growth in a cell viability assay, IC50=3.23473μM SANGER
LC-1F Growth inhibition assay Inhibition of human LC-1F cell growth in a cell viability assay, IC50=3.30326μM SANGER
SU-DHL-1 Growth inhibition assay Inhibition of human SU-DHL-1 cell growth in a cell viability assay, IC50=3.52915μM SANGER
KG-1 Growth inhibition assay Inhibition of human KG-1 cell growth in a cell viability assay, IC50=3.80547μM SANGER
MSTO-211H Growth inhibition assay Inhibition of human MSTO-211H cell growth in a cell viability assay, IC50=3.95028μM SANGER
L-540 Growth inhibition assay Inhibition of human L-540 cell growth in a cell viability assay, IC50=3.95889μM SANGER
HCC1187 Growth inhibition assay Inhibition of human HCC1187 cell growth in a cell viability assay, IC50=4.03307μM SANGER
RL95-2 Growth inhibition assay Inhibition of human RL95-2 cell growth in a cell viability assay, IC50=4.10119μM SANGER
KINGS-1 Growth inhibition assay Inhibition of human KINGS-1 cell growth in a cell viability assay, IC50=4.17422μM SANGER
SCC-15 Growth inhibition assay Inhibition of human SCC-15 cell growth in a cell viability assay, IC50=4.21476μM SANGER
EW-12 Growth inhibition assay Inhibition of human EW-12 cell growth in a cell viability assay, IC50=4.4199μM SANGER
SIMA Growth inhibition assay Inhibition of human SIMA cell growth in a cell viability assay, IC50=4.46019μM SANGER
NCI-H720 Growth inhibition assay Inhibition of human NCI-H720 cell growth in a cell viability assay, IC50=4.7198μM SANGER
HCC1599 Growth inhibition assay Inhibition of human HCC1599 cell growth in a cell viability assay, IC50=4.8017μM SANGER
8-MG-BA Growth inhibition assay Inhibition of human 8-MG-BA cell growth in a cell viability assay, IC50=4.85156μM SANGER
RPMI-6666 Growth inhibition assay Inhibition of human RPMI-6666 cell growth in a cell viability assay, IC50=5.08842μM SANGER
BC-3 Growth inhibition assay Inhibition of human BC-3 cell growth in a cell viability assay, IC50=5.25452μM SANGER
LB996-RCC Growth inhibition assay Inhibition of human LB996-RCC cell growth in a cell viability assay, IC50=5.28958μM SANGER
TE-5 Growth inhibition assay Inhibition of human TE-5 cell growth in a cell viability assay, IC50=5.39519μM SANGER
MPP-89 Growth inhibition assay Inhibition of human MPP-89 cell growth in a cell viability assay, IC50=5.53594μM SANGER
DJM-1 Growth inhibition assay Inhibition of human DJM-1 cell growth in a cell viability assay, IC50=5.63516μM SANGER
LC-2-ad Growth inhibition assay Inhibition of human LC-2-ad cell growth in a cell viability assay, IC50=5.66116μM SANGER
NEC8 Growth inhibition assay Inhibition of human NEC8 cell growth in a cell viability assay, IC50=5.68736μM SANGER
KGN Growth inhibition assay Inhibition of human KGN cell growth in a cell viability assay, IC50=5.69705μM SANGER
MOLT-13 Growth inhibition assay Inhibition of human MOLT-13 cell growth in a cell viability assay, IC50=5.82867μM SANGER
EW-3 Growth inhibition assay Inhibition of human EW-3 cell growth in a cell viability assay, IC50=5.87026μM SANGER
HOP-62 Growth inhibition assay Inhibition of human HOP-62 cell growth in a cell viability assay, IC50=6.06751μM SANGER
EW-22 Growth inhibition assay Inhibition of human EW-22 cell growth in a cell viability assay, IC50=6.09281μM SANGER
EW-11 Growth inhibition assay Inhibition of human EW-11 cell growth in a cell viability assay, IC50=6.27578μM SANGER
EB2 Growth inhibition assay Inhibition of human EB2 cell growth in a cell viability assay, IC50=6.33123μM SANGER
TE-9 Growth inhibition assay Inhibition of human TE-9 cell growth in a cell viability assay, IC50=6.42042μM SANGER
IST-SL2 Growth inhibition assay Inhibition of human IST-SL2 cell growth in a cell viability assay, IC50=6.51935μM SANGER
GB-1 Growth inhibition assay Inhibition of human GB-1 cell growth in a cell viability assay, IC50=6.57311μM SANGER
D-247MG Growth inhibition assay Inhibition of human D-247MG cell growth in a cell viability assay, IC50=6.63417μM SANGER
TK10 Growth inhibition assay Inhibition of human TK10 cell growth in a cell viability assay, IC50=6.64799μM SANGER
A388 Growth inhibition assay Inhibition of human A388 cell growth in a cell viability assay, IC50=6.70097μM SANGER
EHEB Growth inhibition assay Inhibition of human EHEB cell growth in a cell viability assay, IC50=7.13498μM SANGER
ECC4 Growth inhibition assay Inhibition of human ECC4 cell growth in a cell viability assay, IC50=7.2399μM SANGER
HAL-01 Growth inhibition assay Inhibition of human HAL-01 cell growth in a cell viability assay, IC50=7.45581μM SANGER
SR Growth inhibition assay Inhibition of human SR cell growth in a cell viability assay, IC50=7.64918μM SANGER
KU812 Growth inhibition assay Inhibition of human KU812 cell growth in a cell viability assay, IC50=8.02775μM SANGER
YT Growth inhibition assay Inhibition of human YT cell growth in a cell viability assay, IC50=8.11695μM SANGER
MOLT-4 Growth inhibition assay Inhibition of human MOLT-4 cell growth in a cell viability assay, IC50=8.51012μM SANGER
SK-UT-1 Growth inhibition assay Inhibition of human SK-UT-1 cell growth in a cell viability assay, IC50=8.59275μM SANGER
MLMA Growth inhibition assay Inhibition of human MLMA cell growth in a cell viability assay, IC50=8.65529μM SANGER
MFH-ino Growth inhibition assay Inhibition of human MFH-ino cell growth in a cell viability assay, IC50=8.9591μM SANGER
IM-9 Growth inhibition assay Inhibition of human IM-9 cell growth in a cell viability assay, IC50=9.06101μM SANGER
NCI-H322M Growth inhibition assay Inhibition of human NCI-H322M cell growth in a cell viability assay, IC50=9.28598μM SANGER
CESS Growth inhibition assay Inhibition of human CESS cell growth in a cell viability assay, IC50=9.3786μM SANGER
KE-37 Growth inhibition assay Inhibition of human KE-37 cell growth in a cell viability assay, IC50=9.49296μM SANGER
U-87-MG Growth inhibition assay Inhibition of human U-87-MG cell growth in a cell viability assay, IC50=9.78165μM SANGER
EoL-1-cell Growth inhibition assay Inhibition of human EoL-1-cell cell growth in a cell viability assay, IC50=9.93708μM SANGER
CA46 Growth inhibition assay Inhibition of human CA46 cell growth in a cell viability assay, IC50=10.5081μM SANGER
LB1047-RCC Growth inhibition assay Inhibition of human LB1047-RCC cell growth in a cell viability assay, IC50=10.5566μM SANGER
NB1 Growth inhibition assay Inhibition of human NB1 cell growth in a cell viability assay, IC50=10.5731μM SANGER
LS-123 Growth inhibition assay Inhibition of human LS-123 cell growth in a cell viability assay, IC50=10.5844μM SANGER
GOTO Growth inhibition assay Inhibition of human GOTO cell growth in a cell viability assay, IC50=10.966μM SANGER
LB2241-RCC Growth inhibition assay Inhibition of human LB2241-RCC cell growth in a cell viability assay, IC50=11.3688μM SANGER
RPMI-8402 Growth inhibition assay Inhibition of human RPMI-8402 cell growth in a cell viability assay, IC50=11.7395μM SANGER
EW-18 Growth inhibition assay Inhibition of human EW-18 cell growth in a cell viability assay, IC50=12.2119μM SANGER
SF268 Growth inhibition assay Inhibition of human SF268 cell growth in a cell viability assay, IC50=12.5572μM SANGER
NCI-H2171 Growth inhibition assay Inhibition of human NCI-H2171 cell growth in a cell viability assay, IC50=12.7506μM SANGER
SCLC-21H Growth inhibition assay Inhibition of human SCLC-21H cell growth in a cell viability assay, IC50=13.4345μM 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
ES5 Growth inhibition assay Inhibition of human ES5 cell growth in a cell viability assay, IC50=13.9428μM SANGER
KALS-1 Growth inhibition assay Inhibition of human KALS-1 cell growth in a cell viability assay, IC50=14.1325μM SANGER
GI-1 Growth inhibition assay Inhibition of human GI-1 cell growth in a cell viability assay, IC50=14.1988μM SANGER
U-698-M Growth inhibition assay Inhibition of human U-698-M cell growth in a cell viability assay, IC50=14.435μM SANGER
LP-1 Growth inhibition assay Inhibition of human LP-1 cell growth in a cell viability assay, IC50=14.4661μM SANGER
NCI-H23 Growth inhibition assay Inhibition of human NCI-H23 cell growth in a cell viability assay, IC50=14.724μM SANGER
HC-1 Growth inhibition assay Inhibition of human HC-1 cell growth in a cell viability assay, IC50=14.7737μM SANGER
NCI-H1355 Growth inhibition assay Inhibition of human NCI-H1355 cell growth in a cell viability assay, IC50=14.9946μM SANGER
LC4-1 Growth inhibition assay Inhibition of human LC4-1 cell growth in a cell viability assay, IC50=15.1355μM SANGER
CCRF-CEM Growth inhibition assay Inhibition of human CCRF-CEM cell growth in a cell viability assay, IC50=15.2306μM SANGER
TE-1 Growth inhibition assay Inhibition of human TE-1 cell growth in a cell viability assay, IC50=15.5684μM 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
LOXIMVI Growth inhibition assay Inhibition of human LOXIMVI cell growth in a cell viability assay, IC50=16.4329μM SANGER
MONO-MAC-6 Growth inhibition assay Inhibition of human MONO-MAC-6 cell growth in a cell viability assay, IC50=16.6532μM SANGER
NCI-H716 Growth inhibition assay Inhibition of human NCI-H716 cell growth in a cell viability assay, IC50=16.9882μM SANGER
JiyoyeP-2003 Growth inhibition assay Inhibition of human JiyoyeP-2003 cell growth in a cell viability assay, IC50=17.2361μM SANGER
SW954 Growth inhibition assay Inhibition of human SW954 cell growth in a cell viability assay, IC50=17.7495μM SANGER
CAS-1 Growth inhibition assay Inhibition of human CAS-1 cell growth in a cell viability assay, IC50=17.7612μM SANGER
SF539 Growth inhibition assay Inhibition of human SF539 cell growth in a cell viability assay, IC50=17.8653μM SANGER
COLO-800 Growth inhibition assay Inhibition of human COLO-800 cell growth in a cell viability assay, IC50=18.0144μM SANGER
KY821 Growth inhibition assay Inhibition of human KY821 cell growth in a cell viability assay, IC50=18.4608μM SANGER
LU-65 Growth inhibition assay Inhibition of human LU-65 cell growth in a cell viability assay, IC50=18.5947μM SANGER
JVM-2 Growth inhibition assay Inhibition of human JVM-2 cell growth in a cell viability assay, IC50=18.6058μM SANGER
CRO-AP2 Growth inhibition assay Inhibition of human CRO-AP2 cell growth in a cell viability assay, IC50=18.6171μM SANGER
NCI-H128 Growth inhibition assay Inhibition of human NCI-H128 cell growth in a cell viability assay, IC50=19.2368μM SANGER
AM-38 Growth inhibition assay Inhibition of human AM-38 cell growth in a cell viability assay, IC50=19.7389μM SANGER
NCI-H64 Growth inhibition assay Inhibition of human NCI-H64 cell growth in a cell viability assay, IC50=19.9518μM SANGER
ES6 Growth inhibition assay Inhibition of human ES6 cell growth in a cell viability assay, IC50=20.3657μM SANGER
KARPAS-45 Growth inhibition assay Inhibition of human KARPAS-45 cell growth in a cell viability assay, IC50=20.4183μM SANGER
NCI-H1581 Growth inhibition assay Inhibition of human NCI-H1581 cell growth in a cell viability assay, IC50=20.5843μM SANGER
KURAMOCHI Growth inhibition assay Inhibition of human KURAMOCHI cell growth in a cell viability assay, IC50=20.7537μM SANGER
NALM-6 Growth inhibition assay Inhibition of human NALM-6 cell growth in a cell viability assay, IC50=21.2955μM SANGER
DSH1 Growth inhibition assay Inhibition of human DSH1 cell growth in a cell viability assay, IC50=21.3697μM SANGER
Becker Growth inhibition assay Inhibition of human Becker cell growth in a cell viability assay, IC50=21.5612μM 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
HCC2157 Growth inhibition assay Inhibition of human HCC2157 cell growth in a cell viability assay, IC50=22.2184μM 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
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
LS-1034 Growth inhibition assay Inhibition of human LS-1034 cell growth in a cell viability assay, IC50=24.2647μM SANGER
SF126 Growth inhibition assay Inhibition of human SF126 cell growth in a cell viability assay, IC50=24.9217μM SANGER
MC-CAR Growth inhibition assay Inhibition of human MC-CAR cell growth in a cell viability assay, IC50=25.0901μM SANGER
RL Growth inhibition assay Inhibition of human RL cell growth in a cell viability assay, IC50=25.1477μM SANGER
KNS-81-FD Growth inhibition assay Inhibition of human KNS-81-FD cell growth in a cell viability assay, IC50=25.8563μM SANGER
Ramos-2G6-4C10 Growth inhibition assay Inhibition of human Ramos-2G6-4C10 cell growth in a cell viability assay, IC50=26.0093μM SANGER
TE-8 Growth inhibition assay Inhibition of human TE-8 cell growth in a cell viability assay, IC50=26.0599μM SANGER
ES8 Growth inhibition assay Inhibition of human ES8 cell growth in a cell viability assay, IC50=26.1087μM SANGER
SK-PN-DW Growth inhibition assay Inhibition of human SK-PN-DW cell growth in a cell viability assay, IC50=27.3933μM SANGER
NCI-H2126 Growth inhibition assay Inhibition of human NCI-H2126 cell growth in a cell viability assay, IC50=27.6384μM 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
HCE-T Growth inhibition assay Inhibition of human HCE-T cell growth in a cell viability assay, IC50=29.2587μM SANGER
IST-MES1 Growth inhibition assay Inhibition of human IST-MES1 cell growth in a cell viability assay, IC50=29.329μM SANGER
CTB-1 Growth inhibition assay Inhibition of human CTB-1 cell growth in a cell viability assay, IC50=31.889μM SANGER
MOLT-16 Growth inhibition assay Inhibition of human MOLT-16 cell growth in a cell viability assay, IC50=32.0214μM SANGER
BC-1 Growth inhibition assay Inhibition of human BC-1 cell growth in a cell viability assay, IC50=32.527μM SANGER
A253 Growth inhibition assay Inhibition of human A253 cell growth in a cell viability assay, IC50=32.9626μM SANGER
D-336MG Growth inhibition assay Inhibition of human D-336MG cell growth in a cell viability assay, IC50=33.9563μM SANGER
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
Click to View More Cell Line Experimental Data

Biological Activity

Description AZ628 is a new pan-Raf inhibitor for BRAF, BRAFV600E, and c-Raf-1 with IC50 of 105 nM, 34 nM and 29 nM in cell-free assays, also inhibits VEGFR2, DDR2, Lyn, Flt1, FMS, etc. AZ628 induces apoptosis.
Targets
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
In vitro
In vitro

AZ628 prevents activation of number of tyrosine protein kinases including VEGFR2, DDR2, Lyn, Flt1, FMS and others. AZ628 suppresses anchorage-dependent and -independent growth, gives rise to cell cycle arrest, and induces apoptosis in colon and melanoma cell lines harboring B-RafV600E mutation. The profile of AZ628 cross-reactivity suggests that similar to AZ628 may be antiangiogenic based on prevention of VEGFR2. [1] AZ628-resistant clones are approximately 100-fold more resistant to AZ628 than the parental cell line, exhibiting IC50 of approximately 10 μM, compared with 0.1 μM for the parental cell line. Effective suppression of p-ERK1/2 levels is observed in the M14 parental cell line following treatment with increasing concentrations of AZ628. AZ628-resistant clones express elevated CRAF. Elevated CRAF expression is a potential mechanism of acquired resistance to continuous AZ628 exposure, resulting in sustained activation of ERK1/2. p-ERK1/2 activity is not significantly inhibited by exposure to AZ628 in one of these three AZ628-insensitive cell lines (Wm1552C). Unlike in the AZ628-resistant M14 cells in which AZ628 fails to suppress the activation of ERK, AZ628 treatment efficiently attenuates ERK activation in the NRAS mutant melanoma cells.[2]
Cell Research Cell lines M14 expressing the V600E BRAF mutation
Concentrations 0.01-10 μM
Incubation Time Overnight
Method

Approximately 0.5-2.5 × 105 M14 cells are seeded in 12 or 24 - well plates, respectively, in medium supplemented with 5% FBS. After overnight incubation, the cells are treated with various concentrations of AZ628. Fresh medium and drug is replaced every 2 days until the untreated control wells reached confluence. At this time-point, the media is removed and the cells are fixed in 4% formaldehyde in PBS for 20 minutes at room temperature. Cells are then washed twice with PBS and stained with a 1:5000 solution of the fluorescent nucleic acid stain Syto60. Quantitation of fluorescent signal intensity is carried out at 700 nm, using an Odyssey Infrared Imager. Each experiment is performed in quadruplicate and the results shown represent the average of the four values compared to untreated wells. Error bars represent standard deviation of the 4 values from the mean. High-throughput cell growth/viability assays are performed.
Experimental Result Images Methods Biomarkers Images PMID
Western blot p-ERK / ERK / p-MEK / MEK / BIM / BRAF / CRAF 21098728
Growth inhibition assay Cell viability 21098728

Chemical Information & Solubility

Molecular Weight 451.52 Formula

C27H25N5O2
CAS No. 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
Storage (From the date of receipt)

In vitro
Batch:

DMSO : 90 mg/mL ( (199.32 mM) Moisture-absorbing DMSO reduces solubility. Please use fresh DMSO.)

Water : Insoluble

Ethanol : Insoluble


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In vivo
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Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid concentration mg/mL, Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug. )

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Tech Support

Answers to questions you may have can be found in the inhibitor handling instructions. Topics include how to prepare stock solutions, how to store inhibitors, and issues that need special attention for cell-based assays and animal experiments.

Handling Instructions

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