Raf Kinase Inhibitor V - CAS 918505-84-7 - Calbiochem

A cell-permeable azaindole compound that interacts with Raf via both the ATP-binding site and a "Raf-selective pocket" that exhibits conformation-dependent inhibitor-binding modes and accounts for the compound′s preferential binding and inhibitory activity toward the active Raf mutants (IC₅₀ = 6.7, 13, 130, 160, and >1,300 nM against C-Raf-1^Y340D/Y341D, B-Raf^V600E, BRK, WT B-Raf, and 64 other kinases, respectively). Shown to inhibit the proliferation and cellular Erk phosphorylation much more potently in B-Raf^V600E-bearing than WT B-Raf-bearing cancer cell lines in vitro and effectively suppress COLO205-derived tumor growth in mice in vivo (near complete regression during the 1-wk treatment period; 20 mg/kg, daily p.o.).

A cell-permeable azaindole compound that interacts with Raf via both the ATP-binding site and a "Raf-selective pocket" that exhibits conformation-dependent inhibitor-binding modes and accounts for the compound′s preferential binding and inhibitory activity toward the active Raf mutants (IC₅₀ = 6.7, 13, 130, 160, and >1,300 nM against C-Raf-1^Y340D/Y341D, B-Raf^V600E, BRK, WT B-Raf, and 64 other kinases, respectively). Shown to inhibit the proliferation and cellular Erk phosphorylation much more potently in B-Raf^V600E-bearing than WT B-Raf-bearing cancer cell lines in vitro and effectively suppress COLO205-derived tumor growth in mice in vivo (near complete regression during the 1-wk treatment period; 20 mg/kg, daily, p.o.).

Packaged under inert gas

Following reconstitution, aliquot and freeze (-20°C). Stock solutions are stable for up to 3 months at -20°C.

Tsai, J., et al. 2008. Proc. Natl. Acad. Sci. USA105, 3041.

CALBIOCHEM is a registered trademark of Merck KGaA, Darmstadt, Germany

Toxicity: Standard Handling (A)