Raf inhibitor 1 is a potent Raf kinase inhibitor with K i s of 1 nM, 1 nM, and 0.3 nM for B-Raf WT , B-Raf V600E , and C-Raf , respectively. In Vitro Raf inhibitor 1 (Compound 13) inhibits A375 and HCT-116 proliferation with IC 50 s of 0.31 and 0.72 μM, respectively. Raf inhibitor 1 (Compound 13) binds to and stabilizes B-Raf in a DFG-out, inactive conformation in which the ATP pocket is partially filled by Phe595 and Gly596 from the DFG motif. Raf inhibitor 1 (Compound 13) additionally exhibits low micromolar inhibition against wild type B-Raf cell lines, which may be due to off-target kinase activities or alternatively to pan-Raf inhibition, including Raf dimers. MCE has not independently confirmed the accuracy of these methods. They are for reference only. Form:Solid IC50& Target:B-Raf 1 nM (Ki) B-Raf V600E 1 nM (Ki) c-Raf 0.3 nM (Ki)
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Raf inhibitor 1
CAS number：1093100-40-3 molecular formula：C26H19ClN8
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| Chinese alias | Raf 抑制剂 1 | ||
| English alias | - | ||
| CAS number | 1093100-40-3 | molecular formula | C26H19ClN8 |
| molecular weight | 478.9 g/mol | Exact mass | ≥98% |
| PSA | 104.000 Ų | logp | 5.600 |
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