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AZ 628 Raf inibitore

Name: AZ 628
Brand: Selleck Chemicals
SKU: S2746
Rating: 5 (45 reviews)

N. Cat.S2746

AZ628 è un nuovo inibitore pan-Raf per BRAF, BRAFV600E e c-Raf-1 con IC50 di 105 nM, 34 nM e 29 nM in saggi acellulari, inibisce anche VEGFR2, DDR2, Lyn, Flt1, FMS, ecc. AZ628 induce apoptosi.

Struttura chimica

Peso molecolare: 451.52

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Controllo Qualità

Lotto: S274601 DMSO]90 mg/mL]false]Water]Insoluble]false]Ethanol]Insoluble]false Purezza: 99.89%

Citato in Nature Medicine per la sua qualità superiore
COA
NMR
SDS
Scheda tecnica

99.89

Target correlati	ERK p38 MAPK JNK MEK Ras KRas S6 Kinase MAP4K TAK1 Mixed Lineage Kinase
Altro Raf Inibitori	LY3009120 Exarafenib (KIN-2787) GDC-0879 Avutometinib (Ro5126766, CH5126766) PLX-4720 SB590885 TAK-632 GW5074 RAF265 (CHIR-265) PLX8394 (Plixorafenib, FORE8394)

Coltura cellulare, trattamento e concentrazione di lavoro

Linee cellulari	Tipo di saggio	Tempo di incubazione	Descrizione dellattività	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
Clicca per visualizzare più dati sperimentali sulle linee cellulari

Informazioni chimiche, conservazione e stabilità

Peso molecolare	451.52	Formula	C₂₇H₂₅N₅O₂	Conservazione (Dalla data di ricezione)	3 anni-20°Cpolvere
N. CAS	878739-06-1	Scarica SDF		Conservazione delle soluzioni stock	1 anno-80°Cin solvente 1 mese-20°Cin solvente
Sinonimi	N/A			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

Solubilità

In vitro
Lotto:

DMSO : 90 mg/mL (199.32 mM)
(Il DMSO contaminato da umidità può ridurre la solubilità. Utilizzare DMSO fresco e anidro.)

Water : Insoluble

Ethanol : Insoluble

Calcolatore di Molarità

Massa	Concentrazione	Volume	Peso molecolare
=	×	×

Calcolatore di Diluizione Calcolatore del Peso Molecolare

In vivo Lotto:
Homogeneous suspension	CMC-NA	≥5mg/ml	Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.

Calcolatore di formulazione in vivo (Soluzione chiara)

Passo 1: Inserire le informazioni di seguito (Consigliato: Un animale aggiuntivo per tenere conto della perdita durante lesperimento)

Dosaggio: mg/kg Peso medio degli animali: g Volume di dosaggio per animale:μL Numero di animali:

Passo 2: Inserire la formulazione in vivo (Questo è solo il calcolatore, non la formulazione. Contattateci prima se non cè una formulazione in vivo nella sezione Solubilità.)

% DMSO + % + % Tween 80 + % ddH₂O

%DMSO+ %

Risultati del calcolo:

Concentrazione di lavoro: mg/ml;

Metodo per preparare il liquido master di DMSO: mg farmaco predissolto in μL DMSO ( Concentrazione del liquido master mg/mL, Vi preghiamo di contattarci prima se la concentrazione supera la solubilità del DMSO del lotto del farmaco. )

Metodo per preparare la formulazione in vivo: Prendere μL DMSO liquido master, quindi aggiungereμL PEG300, mescolare e chiarire, quindi aggiungereμL Tween 80, mescolare e chiarire, quindi aggiungere μL ddH₂O, mescolare e chiarire.

Metodo per preparare la formulazione in vivo: Prendere μL DMSO liquido master, quindi aggiungere μL Olio di mais, mescolare e chiarire.

Nota: 1. Si prega di assicurarsi che il liquido sia limpido prima di aggiungere il solvente successivo.
2. Assicurarsi di aggiungere il/i solvente/i in ordine. È necessario assicurarsi che la soluzione ottenuta, nellaggiunta precedente, sia una soluzione limpida prima di procedere allaggiunta del solvente successivo. Metodi fisici come il vortex, gli ultrasuoni o il bagno dacqua calda possono essere utilizzati per facilitare la dissoluzione.

Meccanismo dazione

Targets/IC₅₀/Ki	C-Raf-1 (Cell-free assay) 29 nM B-Raf (V600E) (Cell-free assay) 34 nM B-Raf (Cell-free assay) 105 nM
In vitro	AZ628 previene l'attivazione di un certo numero di tirosina protein chinasi inclusi VEGFR2, DDR2, Lyn, Flt1, FMS e altri. AZ628 sopprime la crescita dipendente e indipendente dall'ancoraggio, provoca l'arresto del ciclo cellulare e induce apoptosi in linee cellulari di colon e melanoma che ospitano la mutazione B-RafV600E. Il profilo di reattività crociata di AZ628 suggerisce che, in modo simile, AZ628 potrebbe essere antiangiogenico basandosi sulla prevenzione di VEGFR2. I cloni resistenti a AZ628 sono circa 100 volte più resistenti a AZ628 rispetto alla linea cellulare parentale, esibendo una IC50 di circa 10 μM, rispetto a 0,1 μM per la linea cellulare parentale. Una soppressione efficace dei livelli di p-ERK1/2 viene osservata nella linea cellulare parentale M14 in seguito al trattamento con concentrazioni crescenti di AZ628. I cloni resistenti a AZ628 esprimono CRAF elevato. L'espressione elevata di CRAF è un potenziale meccanismo di resistenza acquisita all'esposizione continua a AZ628, con conseguente attivazione sostenuta di ERK1/2. L'attività di p-ERK1/2 non è significativamente inibita dall'esposizione a AZ628 in una di queste tre linee cellulari insensibili a AZ628 (Wm1552C). A differenza delle cellule M14 resistenti a AZ628 in cui AZ628 non riesce a sopprimere l'attivazione di ERK, il trattamento con AZ628 attenua efficacemente l'attivazione di ERK nelle cellule di melanoma mutanti NRAS.
Riferimenti	[1] https://pubmed.ncbi.nlm.nih.gov/18020980/ [2] https://pubmed.ncbi.nlm.nih.gov/18559533/

Applicazioni

Metodi	Biomarcatori	Immagini	PMID
Western blot	p-ERK / ERK / p-MEK / MEK / BIM / BRAF / CRAF		21098728
Growth inhibition assay	Cell viability		21098728

Supporto tecnico

Istruzioni per la manipolazione

Tel: +1-832-582-8158 Ext:3

Per qualsiasi altra domanda, si prega di lasciare un messaggio.

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C5=C4/X	C5:	LOG(C5):
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