AZ 628

Names

[ Name ]:
AZ 628

[Synonym ]:
cc-82
Benzamide, 3-(1-cyano-1-methylethyl)-N-[3-[(3,4-dihydro-3-methyl-4-oxo-6-quinazolinyl)amino]-4-methylphenyl]-
AZ628
3-(2-Cyano-2-propanyl)-N-{4-methyl-3-[(3-methyl-4-oxo-3,4-dihydro-6-quinazolinyl)amino]phenyl}benzamide
AZ 628

Biological Activity

[Description]:

AZ628 is a pan-Raf kinase inhibitor with IC50s of 105, 34 and 29 nM for B-Raf, B-RafV600E, and c-Raf-1, respectively.

[Related Catalog]:

Signaling Pathways >> MAPK/ERK Pathway >> Raf

Research Areas >> Cancer

[Target]

c-Raf-1:29 nM (IC50)

B-RafV600E:34 nM (IC50)

B-Raf:105 nM (IC50)

[In Vitro]

AZ628 reduces activities of preactivated B-Raf, B-RafV600E, and c-Raf-1 in in vitro kinase assays, with IC50 values of 105, 34 and 29 nM, respectively. AZ628 also inhibits activation of number of tyrosine protein kinases including VEGFR2, DDR2, Lyn, Flt1, FMS and others. AZ628 inhibits anchorage-dependent and -independent growth, causes cell cycle arrest, and induces apoptosis in colon and melanoma cell lines harboring B-RafV600E mutation[1]. AZ-628 suppresses growth in cells expressing K-RASG13D. Inhibition of RAF with AZ-628 suppresses MEK and ERK phosphorylation. AZ-628 selectively affects viability in K-RAS mutant cells[2].

[Cell Assay]

Cell viability quantified by Syto60 after 72 hours of AZ-628 (0.5, 1.0, and 1.5 μM), CI-1040 or BAY61-3606 treatment in HCT-116 (K-RASG13D/+) or HKe-3 (K-RAS-/+) cell lines. Relative cell viability is normalized to DMSO vehicle treated control for each cell line[2].

[References]

[1]. Khazak V, et al. Selective Raf inhibition in cancer therapy. Expert Opin Ther Targets. 2007 Dec;11(12):1587-609.

[2]. Lau KS, et al. BAY61-3606 affects the viability of colon cancer cells in a genotype-directed manner. PLoS One. 2012;7(7):e41343.

[Related Small Molecules]

PLX8394 | Doramapimod (BIRB 796) | PLX-4720 | LGX 818 | LY 3009120 | GW5074 | RAF265 (CHIR-265) | RAF709 | CEP-32496 | GDC-0879 | LXH254 | TAK-632 | PLX7904 | HG6-64-1 | RO 5126766

Chemical & Physical Properties

[ Density]:
1.2±0.1 g/cm3

[ Molecular Formula ]:
C₂₇H₂₅N₅O₂

[ Molecular Weight ]:
451.520

[ Exact Mass ]:
451.200836

[ PSA ]:
99.81000

[ LogP ]:
2.78

[ Appearance of Characters ]:
white to beige

[ Index of Refraction ]:
1.638

[ Storage condition ]:
?20°C

[ Water Solubility ]:
DMSO: soluble10mg/mL, clear

MSDS

Click to get detail MSDS

Safety Information

[ Symbol ]:

GHS06

[ Signal Word ]:
Danger

[ Hazard Statements ]:
H301-H315-H319-H335

[ Precautionary Statements ]:
P261-P301 + P310-P305 + P351 + P338

[ Hazard Codes ]:
T

[ Risk Phrases ]:
25-36/37/38

[ Safety Phrases ]:
26-36/37/39-45

[ RIDADR ]:
UN 2811 6.1 / PGIII

[ Hazard Class ]:
6.1

[ HS Code ]:
2933990090

Customs

[ HS Code ]: 2933990090

[ Summary ]:
2933990090. heterocyclic compounds with nitrogen hetero-atom(s) only. VAT:17.0%. Tax rebate rate:13.0%. . MFN tariff:6.5%. General tariff:20.0%