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B-Raf inhibitor 1

Names

[ CAS No. ]:
1093100-40-3

[ Name ]:
B-Raf inhibitor 1

[Synonym ]:
L1E
B-Raf inhibitor 1
N-(4-Chlorophenyl)-6-methyl-N-[3-(1H-purin-6-yl)-2-pyridinyl]-1,5-isoquinolinediamine
1,5-Isoquinolinediamine, N-(4-chlorophenyl)-6-methyl-N-[3-(9H-purin-6-yl)-2-pyridinyl]-
3idp
pyridylpurine aminoisoquinoline,1

Biological Activity

[Description]:

B-Raf inhibitor 1 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]:

Research Areas >> Cancer

[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]

[1]. Wang X, et al. Conformation-specific effects of Raf kinase inhibitors. J Med Chem. 2012 Sep 13;55(17):7332-41.


[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

[ Density]:
1.5±0.1 g/cm3

[ Boiling Point ]:
735.4±60.0 °C at 760 mmHg

[ Molecular Formula ]:
C26H19ClN8

[ Molecular Weight ]:
478.936

[ Flash Point ]:
398.6±32.9 °C

[ Exact Mass ]:
478.142120

[ PSA ]:
104.30000

[ LogP ]:
4.97

[ Vapour Pressure ]:
0.0±2.4 mmHg at 25°C

[ Index of Refraction ]:
1.798

[ Storage condition ]:
2-8℃

Related Compounds