A quinazilinone that inhibits several Raf kinases

AZ 628 – 1 mg

Brand:
Cayman
CAS:
878739-06-1
Storage:
-20
UN-No:
De Minimis - 2811 / 6.1

The Raf kinases activate cellular pathways that lead to cell proliferation and can contribute to certain types of cancer.{19941,24815} Mutations in the kinase B-Raf are involved in a wide range of cancers.{18549,22622} In particular, the mutation B-RafV600E occurs in melanomas and other types of cancer but is poorly targeted by many inhibitors of wild type B-Raf.{24813,24814} AZ 628 is a quinazilinone that inhibits several Raf kinases, including B-Raf, B-RafV600E, and c-Raf-1 (IC50s = 105, 34, and 29 nM in in vitro kinase assays).{27947,27948} It also prevents activation of several tyrosine kinases, including VEGFR2, DDR2, Lyn, Flt1, and FMS.{27947} In colon and melanoma cell lines carrying B-RafV600E mutations, AZ 628 is reported to inhibit anchorage-dependent and -independent growth, induce cell cycle arrest, and cause apoptosis.{27947}  

 

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Description

A quinazilinone that inhibits several Raf kinases, including B-Raf, B-RafV600E, and c-Raf-1 (IC50s = 105, 34, and 29 nM in vitro); inhibits anchorage-dependent and -independent growth, induces cell cycle arrest, and causes apoptosis in colon and melanoma cell lines carrying B-RafV600E mutations

Formal name: 3-(1-cyano-1-methylethyl)-N-[3-[(3,4-dihydro-3-methyl-4-oxo-6-quinazolinyl)amino]-4-methylphenyl]-benzamide

Synonyms: 

Molecular weight: 451.5

CAS: 878739-06-1

Purity: ≥98%

Formulation: A crystalline solid

Product Type|Biochemicals|Kinase Inhibitors|RAS/RAF/MEK/ERK/MAPK||Product Type|Biochemicals|Small Molecule Inhibitors|Kinases||Research Area|Cancer|Cell Cycle||Research Area|Cancer|Cell Death|Apoptosis||Research Area|Cancer|Cell Migration & Metastasis||Research Area|Cancer|Cell Signaling|Growth Factor Receptor Signaling

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