LY3009120 (DP-4978)

Description: LY03009120 (DP4978; LY-3009120; LY-03009120; DP-4978) is a novel and potent pan-Raf inhibitor with potential anticancer activity. It inhibits A-raf, B-Raf, and C-Raf with IC50s of 44 nM, 37 nM, and 42 nM, respectively. It has potent antitumor activity and showed activities against BRaf or Ras mutant tumor cells. It binds to ARaf, BRaf and CRaf isoforms with similar affinity in cells with activating mutations of BRaf or KRas. LY3009120 inhibits MEK phosphorylation and cell proliferation in vitro, and exhibits anti-tumor activity in multiple xenograft models carrying mutations in BRaf, NRas or KRas.

References: 1 J Med Chem. 2015, 58(10), 4165-4179. 2 Chem Biol.011, 18(6), 699-710.