TAK-632

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). It demonstrates 14-1,200-fold selectivity for Raf over a panel of 26 different kinases. 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.Formal Name: N-[5-[[7-cyano-2-[(cyclopropylcarbonyl)amino]-6-benzothiazolyl]oxy]-2-fluorophenyl]-3-(trifluoromethyl)-benzeneacetamide. CAS Number: 1228591-30-7. Molecular Formula: C27H18F4N4O3S. Formula Weight: 554.5. Purity: >98%. Formulation: (Request formulation change), A crystalline solid. Solubility: DMF: 30 mg/ml, DMSO: 30 mg/ml, DMSO:PBS(pH 7.2) (1:4): 0.2 mg/ml, Ethanol: 0.5 mg/ml. lambdamax: 238, 260, 282, 326 nm. SMILES: O=C(NC1=C(F)C=CC(OC2=CC=C(N=C(NC(C3CC3)=O)S4)C4=C2C#N)=C1)CC5=CC(C(F)(F)F)=CC=C5. InChi Code: InChI=1S/C27H18F4N4O3S/c28-19-7-6-17(12-21(19)33-23(36)11-14-2-1-3-16(10-14)27(29,30)31)38-22-9-8-20-24(18(22)13-32)39-26(34-20)35-25(37)15-4-5-15/h1-3,6-10,12,15H,4-5,11H2,(H,33,36)(H,34,35,37). InChi Key: OJFKUJDRGJSAQB-UHFFFAOYSA-N.