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  • DC Chemicals Limited
  • China
  • Product Name: AZ-628
  • Price: $450.0/100mg $900.0/250mg $1800.0/1g
  • Purity: 98.0%
  • Stocking Period: 3 Day
  • Contact: Tony Cao

878739-06-1

878739-06-1 structure
878739-06-1 structure
  • Name: AZ 628
  • Chemical Name: 3-(2-cyanopropan-2-yl)-N-[4-methyl-3-[(3-methyl-4-oxoquinazolin-6-yl)amino]phenyl]benzamide
  • CAS Number: 878739-06-1
  • Molecular Formula: C27H25N5O2
  • Molecular Weight: 451.520
  • Catalog: Biochemical Inhibitor Mitogen-activated protein kinase (MAPK) Raf inhibitor
  • Create Date: 2019-01-01 08:23:33
  • Modify Date: 2024-01-14 16:48:48
  • 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.

Name 3-(2-cyanopropan-2-yl)-N-[4-methyl-3-[(3-methyl-4-oxoquinazolin-6-yl)amino]phenyl]benzamide
Synonyms 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
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
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.

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 white to beige
Index of Refraction 1.638
Storage condition ?20°C
Water Solubility DMSO: soluble10mg/mL, clear
Symbol GHS06
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
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%