产品
编 号：F086146
分子式：C29H31Cl2F3N4O3
分子量：611.48
分子式：C29H31Cl2F3N4O3
分子量：611.48
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CAS No: 1237536-18-3
产品详情
生物活性：
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.
体内研究：
ML786 (75 mg/kg; p.o. once daily for 21 d) inhibits the subcutaneous A375 M xenografts in immunocompromised mice.ML786 (75 mg/kg; a single p.o.) strongly inhibits the Raf pathway in mice.ML786 (10 mg/kg; p.o.) exhibits oral bioavailability of 85% and AUC1-24h of 35.9 μM·h in rats.ML786 (1 mg/kg; i.v.) exhibits plasma clearance of 0.44 L/h/kg and Vss of 3.93 L/kg in rats.Animal Model:Nude NCR (ν/ν) mice bearing A375 M xenografts
Dosage:75 mg/kg
Administration:P.o. once daily for 21 days
Result:Induced partial regressions of the tumor xenografts.Showed no indication of toxicity or weight loss.
体外研究：
ML786 (3 h) inhibits the kinase phosphorylation of extracellular signal-regulated kinase (ERK) (pERK) in A375 cells, with an IC50 of 60 nM.
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.
体内研究：
ML786 (75 mg/kg; p.o. once daily for 21 d) inhibits the subcutaneous A375 M xenografts in immunocompromised mice.ML786 (75 mg/kg; a single p.o.) strongly inhibits the Raf pathway in mice.ML786 (10 mg/kg; p.o.) exhibits oral bioavailability of 85% and AUC1-24h of 35.9 μM·h in rats.ML786 (1 mg/kg; i.v.) exhibits plasma clearance of 0.44 L/h/kg and Vss of 3.93 L/kg in rats.Animal Model:Nude NCR (ν/ν) mice bearing A375 M xenografts
Dosage:75 mg/kg
Administration:P.o. once daily for 21 days
Result:Induced partial regressions of the tumor xenografts.Showed no indication of toxicity or weight loss.
体外研究：
ML786 (3 h) inhibits the kinase phosphorylation of extracellular signal-regulated kinase (ERK) (pERK) in A375 cells, with an IC50 of 60 nM.
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