878739-06-1 in bulk...

878739-06-1 in bulk supply 878739-06-1 in stock AZ-628 good supplier
878739-06-1 in bulk supply 878739-06-1 in stock AZ-628 good supplier

878739-06-1 in bulk supply 878739-06-1 in stock AZ-628 good supplier

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  • Min.Order :1 Gram
  • Purity: 98%
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878739-06-1 in bulk supply 878739-06-1 in stock AZ-628 good supplier

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  • Appearance:Powder
  • Application:Scientific research
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  • ProductionCapacity:1000|Gram|Week
  • Storage:keep sealed and keep from direct light
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878739-06-1 in bulk supply 878739-06-1 in stock AZ-628 good supplier

AZ 628 is a potent, ATP-competitive inhibitor of Raf kinases (IC50 values are 29, 34 and 105 nM for c-Raf1, B-RafV600E and wild-type B-Raf, respectively). Displays selectivity for Raf kinases over a panel of 150 other kinases; inhibits activation of tyrosine protein kinases such as VEGFR2, Lyn, Flt1 and Fms. Also inhibits growth, and induces cell cycle arrest and apoptosis in colon and melanoma cell lines with the B-RafV600E mutation.

AZ628 is a potent tyrosine protein inhibitor to wild-type Raf-1 and Raf-B V600E with IC50 of 29 nM and 34 nM, respectively.

The Raf kinases activate cellular pathways that lead to cell proliferation and can contribute to certain types of cancer. Mutations in the kinase B-Raf are involved in a wide range of cancers. 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. 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). It also prevents activation of several tyrosine kinases, including VEGFR2, DDR2, Lyn, Flt1, and FMS. 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.

Details:

Alternate Name AZ 628; AZ628; AZ-628; 3-(2-cyanopropan-2-yl)-N-[4-methyl-3-[(3-methyl-4-oxoquinazolin-6-yl)amino]phenyl]benzamide
Appearance Solid
CAS # 878739-06-1
Molecular Formula C??H??N?O?
Molecular Weight 451.53
Purity >98%
Solubility DMSO
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
InChi InChI=1S/C27H25N5O2/c1-17-8-9-21(31-25(33)18-6-5-7-19(12-18)27(2,3)15-28)14-24(17)30-20-10-11-23-22(13-20)26(34)32(4)16-29-23/h5-14,16,30H,1-4H3,(H,31,33)
InChi Key ZGBGPEDJXCYQPH-UHFFFAOYSA-N
PubChem CID 11676786
MDL Number MFCD17392577
Handling Protect from air and light
Storage Conditions -20°C
Shipping Conditions Gel Pack

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