ML786 (dihydrochloride)

ML786 dihydrochloride is a potent and orally bioavailable Raf inhibitor, with IC₅₀s of 2.1, 4.2, and 2.5 nM for ^V600EΔB-Raf, wt B-Raf, and C-Raf, respectively. ML786 dihydrochloride also inhibits Abl-1, DDR2, EPHA2, KDR, and RET (IC₅₀=<0.5, 7.0, 11, 6.2, 0.8 nM). ML786 dihydrochloride can be used for the research of cancers^[1]. In Vitro:ML786 (3 h) inhibits the kinase phosphorylation of extracellular signal-regulated kinase (ERK) (pERK) in A375 cells, with an IC₅₀ of 60 nM^[1]. In Vivo:ML786 (75 mg/kg; p.o. once daily for 21 d) inhibits the subcutaneous A375 M xenografts in immunocompromised mice^[1].
ML786 (75 mg/kg; a single p.o.) strongly inhibits the Raf pathway in mice^[1].
ML786 (10 mg/kg; p.o.) exhibits oral bioavailability of 85% and AUC_1-24h of 35.9 μM·h in rats^[1].
ML786 (1 mg/kg; i.v.) exhibits plasma clearance of 0.44 L/h/kg and Vss of 3.93 L/kg in rats^[1].