Stemcell, 73072, Dabrafenib

Dabrafenib is a reversible, selective, and ATP-competitive inhibitor of B-RAF with higher potency towards V600E mutant B-RAF over wild-type B-RAF or C-RAF, with IC₅₀ values of 0.8, 3.2 and 5 nM, respectively (Laquerre et al.; Menzies et al.).

CANCER RESEARCH

· Decreases ERK phosphorylation and inhibits cell proliferation in cells expressing the B-RAF mutation V600E. Prevents tumor growth in mouse xenograft models of B-RAF(V600E) human melanoma and colon cancer (Rheault et al.).

DISEASE MODELING

· Alleviates acetaminophen-induced liver injury through distinct nanomolar inhibition of receptor-interacting protein (RIP3) in mice (Li et al.).