B-Raf inhibitor 1 (dihydrochloride)
Names
[ CAS No. ]:
1191385-19-9
[ Name ]:
B-Raf inhibitor 1 (dihydrochloride)
[Synonym ]:
B-Raf inhibitor 1 dihydrochloride
B-Raf inhibitor 1 (dihydrochloride)
Biological Activity
[Description]:
B-Raf inhibitor 1 dihydrochloride is a potent Raf kinase inhibitor with Kis of 1 nM, 1 nM, and 0.3 nM for B-RafWT, B-RafV600E, and C-Raf, respectively.
[Related Catalog]:
[Target]
B-Raf:1 nM (Ki)
B-RafV600E:1 nM (Ki)
c-Raf:0.3 nM (Ki)
[In Vitro]
B-Raf inhibitor 1 (Compound 13) inhibits A375 and HCT-116 proliferation with IC50s of 0.31 and 0.72 μM, respectively. B-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. B-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[1].
[References]
[Related Small Molecules]
PLX8394
|
Doramapimod (BIRB 796)
|
PLX-4720
|
LGX 818
|
LY 3009120
|
GW5074
|
RAF265 (CHIR-265)
|
AZ 628
|
RAF709
|
CEP-32496
|
GDC-0879
|
LXH254
|
TAK-632
|
PLX7904
|
HG6-64-1
Chemical & Physical Properties
[ Molecular Formula ]:
C26H21Cl3N8
[ Molecular Weight ]:
551.85800
[ Exact Mass ]:
550.09500
[ PSA ]:
104.30000
[ LogP ]:
8.16210
[ Storage condition ]:
2-8℃