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].

ML786 (3 h) inhibits the kinase phosphorylation of extracellular signal-regulated kinase (ERK) (pERK) in A375 cells, with an IC₅₀ of 60 nM^[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

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].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

611.48

C₂₉H₃₁Cl₂F₃N₄O₃

1237536-18-3

O=C(CC1)NC2=C1C(OC3=CC=C(CC[C@@H](NC(C4=CC(C(F)(F)F)=CC(C(C)(C)N)=C4)=O)C5)C5=C3)=CC=N2.Cl.Cl

Room temperature in continental US; may vary elsewhere.

Please store the product under the recommended conditions in the Certificate of Analysis.

• [1]. Gould AE, et, al. Design and optimization of potent and orally bioavailable tetrahydronaphthalene Raf inhibitors. J Med Chem. 2011 Mar 24;54(6):1836-46.  [Content Brief]