产品
编 号：F690440
分子式：C20H17F2N3O3
分子量：385.36
分子式：C20H17F2N3O3
分子量：385.36
产品类型
规格
价格
是否有货
1mg
询价
询价
5mg
询价
询价
10mg
询价
询价
结构图
CAS No: 1464842-09-8
产品详情
生物活性：
M8891 is an orally active, reversible and brain penetrant Methionine Aminopeptidase-2 (MetAP-2) inhibitor with an IC50 of 54 nM and a Ki of 4.33 nM. M8891 does not inhibit MetAP-1 (IC50>10 μM). M8891 inhibits growth of primary endothelial cells as well as tumor cells and demonstrates antiangiogenic and antitumoral activity.
体内研究：
M8891 (po; 20 mg/kg; once a day for 14 days) exhibits strong tumor growth inhibition. M8891 (iv; 0.2 mg/kg) shows low clearance (CL ~0.03-0.4 L/h/kg corresponding to ~1-6% of the liver blood-flow), small to medium volume of distribution (Vss ~0.23-1.3 L/kg), and medium to high oral bioavailability (F ~40-80%). Animal Model:Female CD-1 nude mice aged 6-7 weeks with human U87-MG glioblastoma
Dosage:20 mg/kg
Administration:Po; once a day for 14 days
Result:Exhibited strong tumor growth inhibition.
Animal Model:Rat, dog and monkey
Dosage:0.2 mg/kg (Pharmacokinetic Analysis)
Administration:IV
Result:Showed low clearance (CL ~0.03-0.4 L/h/kg corresponding to ~1-6% of the liver blood-flow), small to medium volume of distribution (Vss ~0.23-1.3 L/kg), and medium to high oral bioavailability (F ~40-80%).
体外研究：
M8891 has an IC50 of 20 nM for HUVEC proliferation.
M8891 is an orally active, reversible and brain penetrant Methionine Aminopeptidase-2 (MetAP-2) inhibitor with an IC50 of 54 nM and a Ki of 4.33 nM. M8891 does not inhibit MetAP-1 (IC50>10 μM). M8891 inhibits growth of primary endothelial cells as well as tumor cells and demonstrates antiangiogenic and antitumoral activity.
体内研究：
M8891 (po; 20 mg/kg; once a day for 14 days) exhibits strong tumor growth inhibition. M8891 (iv; 0.2 mg/kg) shows low clearance (CL ~0.03-0.4 L/h/kg corresponding to ~1-6% of the liver blood-flow), small to medium volume of distribution (Vss ~0.23-1.3 L/kg), and medium to high oral bioavailability (F ~40-80%). Animal Model:Female CD-1 nude mice aged 6-7 weeks with human U87-MG glioblastoma
Dosage:20 mg/kg
Administration:Po; once a day for 14 days
Result:Exhibited strong tumor growth inhibition.
Animal Model:Rat, dog and monkey
Dosage:0.2 mg/kg (Pharmacokinetic Analysis)
Administration:IV
Result:Showed low clearance (CL ~0.03-0.4 L/h/kg corresponding to ~1-6% of the liver blood-flow), small to medium volume of distribution (Vss ~0.23-1.3 L/kg), and medium to high oral bioavailability (F ~40-80%).
体外研究：
M8891 has an IC50 of 20 nM for HUVEC proliferation.
产品资料
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