A selective slow off-rate inhibitor of Raf kinases (IC50s = 8.3

TAK-632 – 1 mg

Brand:
Cayman
CAS:
1228591-30-7
Storage:
-20
UN-No:
Non-Hazardous - /

TAK-632 is a slow off-rate inhibitor of Raf kinases (IC50s = 8.3, 2.4, and 1.4 nM for wild type B-Raf, mutant B-RafV600E, and c-Raf, respectively).{28688} It demonstrates 14-1,200-fold selectivity for Raf over a panel of 26 different kinases.{28688} TAK-632 shows significant antiproliferative activity against mutated B-Raf or mutated N-Ras cancer cell lines and xenograft models, inhibiting MEK phosphorylation with an IC50 value of 12 nM and downstream ERK phosphorylation with an IC50 value of 16 nM.{28688,28689}  

 

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Description

A selective slow off-rate inhibitor of Raf kinases (IC50s = 8.3, 2.4, and 1.4 nM for wild type B-Raf, mutant B-RafV600E, and c-Raf, respectively); shows significant antiproliferative activity against mutated BRAF or mutated NRAS cancer cell lines and xenograft models

Formal name: N-[5-[[7-cyano-2-[(cyclopropylcarbonyl)amino]-6-benzothiazolyl]oxy]-2-fluorophenyl]-3-(trifluoromethyl)-benzeneacetamide

Synonyms: 

Molecular weight: 554.5

CAS: 1228591-30-7

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 Signaling|ERK/MAPK Signaling

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