B-Raf inhibitor 1 Chemical Properties

Boiling point:

735.4±60.0 °C(Predicted)

Density 

1.461±0.06 g/cm3(Predicted)

storage temp. 

Store at -20°C

solubility 

≥ 47.9mg/mL in DMSO

form 

Solid

pka

8.41±0.10(Predicted)

color 

Light yellow to yellow

Safety Information

HS Code 

2933998090

B-Raf inhibitor 1 Usage And Synthesis

Uses

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.

Biological Activity

B-Raf inhibitor 1 is a potent Raf kinase inhibitor for B-RafWT, B-RafV600E, and C-Raf with Ki of 1 nM, 1 nM, and 0.3 nM, 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.

target

IC 50

B-Raf: 1 nM (Ki); B-Raf^V600E: 1 nM (Ki); c-Raf: 0.3 nM (Ki)

References

[1] Wang X, et al. Conformation-specific effects of Raf kinase inhibitors. J Med Chem. 2012 Sep 13;55(17):7332-41. DOI:10.1021/jm300613w

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