BI-882370

BI-882370 is an orally bioavailable RAF inhibitor with IC₅₀ values of 0.8, 0.8, and 0.6 nM for B-RAF^V600E, wild-type B-RAF, and C-RAF in the DFG-out inactive conformation, respectively.¹ It is selective for RAF over a panel of kinases, including LCK, KIT, Src, LYNA, LYNB, and PDGFR (IC₅₀s = 49, 415, 485, 750, 715, and 1,220 nM, respectively). It inhibits proliferation of human B-RAF-mutant melanoma cells when used at concentrations ranging from 1 to 10 nM. It reduces tumor growth in multiple B-RAF-mutant melanoma and colorectal carcinoma mouse xenograft models when administered at a dose of 25 mg/kg twice per day. BI-882370, alone and in combination with trametinib (Item No. 16292), induces tumor regression in an A375 melanoma mouse xenograft model with no resistance developing within three or five weeks, respectively.

WARNING This product is not for human or veterinary use.

1. Waizenegger, I.C., Baum, A., Steurer, S., et al. A novel RAF kinase inhibitor with DFG-out-binding mode: High efficacy in BRAF-mutant tumor xenograft models in the absence of normal tissue hyperproliferation. Mol. Cancer. Ther. 15(3), 354-365 (2016).