B-Raf inhibitor 1 dihydrochloride
B-Raf inhibitor 1 is an inhibitor of B-Raf kinase with IC50 values of 0.31μM and 0.72μM for cell proliferation, respectively in A375 and HCT116.
B-Raf is important in signal transduction and some mutant B-Raf occurs in cancer cells. The most common mutation of these is V600E, which makes B-Raf kinase constitutively active. B-Raf inhibitor 1 belongs to the type IIA inhibitors and binds to the DFG-out ATP-binding site of B-Raf. The selectivity of B-Raf inhibitor 1 is less than of other type inhibitors. Besides mutant B-Raf, it can also inhibit wild type B-Raf and other tyrosine kinase. In cells with wild type B-Raf, B-Raf inhibitor 1 can activate the RAF-MEK-ERK signaling pathway via Raf dimerization. The preclinical toxicity test shows B-Raf inhibitor 1 can induce hyperplasia in a mouse model.
B-Raf is important in signal transduction and some mutant B-Raf occurs in cancer cells. The most common mutation of these is V600E, which makes B-Raf kinase constitutively active. B-Raf inhibitor 1 belongs to the type IIA inhibitors and binds to the DFG-out ATP-binding site of B-Raf. The selectivity of B-Raf inhibitor 1 is less than of other type inhibitors. Besides mutant B-Raf, it can also inhibit wild type B-Raf and other tyrosine kinase. In cells with wild type B-Raf, B-Raf inhibitor 1 can activate the RAF-MEK-ERK signaling pathway via Raf dimerization. The preclinical toxicity test shows B-Raf inhibitor 1 can induce hyperplasia in a mouse model.
| Supplier | BOC Sciences |
|---|---|
| Product # | 1191385-19-9 |
| Pricing | Inquire |
| Cas | 1191385-19-9 |
| Molecular Weight | 551.86 |
| Molecular Formula | C26H21Cl3N8 |
| Canonical SMILES | CC1=C(C2=C(C=C1)C(=NC=C2)NC3=CC=C(C=C3)Cl)NC4=C(C=CC=N4)C5=C6C(=NC=N5)N=CN6.Cl.Cl |