An inhibitor of B-RAF and C-RAF
Belvarafenib is an inhibitor of B-RAF and C-RAF (IC50s = 41, 7, and 2 nM for wild-type B-RAF, B-RAFV600E, and wild-type C-RAF, respectively).1 It is cytotoxic to B-RAFV600E-expressing A375 and SK-MEL-28 melanoma cells (IC50s = 57 and 69 nM, respectively), as well as COLO 205 and HCT116 colon and B-CPAP and CAL-62 thyroid cancer cells (IC50s = 116, 65, 43, and 479 nM, respectively). Belvarafenib reduces tumor growth in A375, SK-MEL-28, SK-MEL-2, and SK-MEL-30 mouse xenograft models.
1.Man, R.-J., Zhang, Y.-L., Jiang, A.-Q., et al.A patent review of RAF kinase inhibitors (2010-2018)Expert Opin. Ther. Pat.29(9)675-688(2019)
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