compound introduction
Information Naporafenib (LXH254) is a type II ATP-competitive inhibitor that inhibits bothB- and CRAF kinaseactivities at picomolar concentrations with a high degree of selectivity against a panel of 456 human kinases and in cell-based assays. Targets B-Raf ; C-Raf In vitro LXH254 not only inhibits MAPK signaling activity in tumor models harboring BRAFV600 mutation, but also inhibits mutant N- and KRAS-driven signaling due to its ability to inhibit both RAF monomers and dimers with similar potencies. LXH254 is orally bioavailable, demonstrates a direct PK/PD relationship and causes tumor regression in multiple cell line and primary human tumor derived xenograft models at well-tolerated doses.
