产品
编 号：F752361
分子式：C22H25ClFN5O2
分子量：445.92
分子式：C22H25ClFN5O2
分子量：445.92
产品类型
规格
价格
是否有货
结构图
CAS No: 2413804-83-6
产品详情
生物活性：
HPK1-IN-21 is a potent inhibitor of HPK1 kinase inhibitor (Ki=0.8 nM). HPK1-IN-21 also has orally active.
体内研究：
HPK1-IN-21 (1, 25 mg/kg) shows 13% oral bioavailability in mouse when oral dose used 25 mg/kg.Pharmacokinetic Parameters of HPK1-IN-21 in mice.compdLM H/R/Ma,dHep H/R/Mb,dmouse iv CL,Vsscmouse F%c
256.9/8.7/389.5/18/3357,1.913%
aLM = Liver microsome predicted clearance (mL/min/kg), H =human, R = rat, M = mouse. bHep = Hepatocyte clearance measuredin mL/min/kg, H = human, R = rat, M = mouse. cMouse PK:C57BL/6, 1 mg/kg iv dose or 25 mg/kg po dose, blood clearance measured in mL/min/kg, Vss = volume of distribution (L/kg). dHLM and Hep clearance values represent arithmetic means of two determinations.Six female (6-9 weeks) C57BL/6 mice, 15-25 g, 1 mg/kg iv (solution in 35% PEG400 in water); 25 mg/kg po (suspension in 0.5% methylcellulose, 0.2% Tween in water)Animal Model:Six female (6-9 weeks) C57BL/6 mice, 15-25 g
Dosage:1, 25 mg/kg
Administration:
Result:Showed 13% oral bioavailability in mice when oral dose used 25 mg/kg.
体外研究：
HPK1-IN-21 (compound 25) (0.001, 0.01, 0.1, 1, 10, 100 μM; 4 hours) inhibits the activity of HPK1 kinase.
HPK1-IN-21 is a potent inhibitor of HPK1 kinase inhibitor (Ki=0.8 nM). HPK1-IN-21 also has orally active.
体内研究：
HPK1-IN-21 (1, 25 mg/kg) shows 13% oral bioavailability in mouse when oral dose used 25 mg/kg.Pharmacokinetic Parameters of HPK1-IN-21 in mice.compdLM H/R/Ma,dHep H/R/Mb,dmouse iv CL,Vsscmouse F%c
256.9/8.7/389.5/18/3357,1.913%
aLM = Liver microsome predicted clearance (mL/min/kg), H =human, R = rat, M = mouse. bHep = Hepatocyte clearance measuredin mL/min/kg, H = human, R = rat, M = mouse. cMouse PK:C57BL/6, 1 mg/kg iv dose or 25 mg/kg po dose, blood clearance measured in mL/min/kg, Vss = volume of distribution (L/kg). dHLM and Hep clearance values represent arithmetic means of two determinations.Six female (6-9 weeks) C57BL/6 mice, 15-25 g, 1 mg/kg iv (solution in 35% PEG400 in water); 25 mg/kg po (suspension in 0.5% methylcellulose, 0.2% Tween in water)Animal Model:Six female (6-9 weeks) C57BL/6 mice, 15-25 g
Dosage:1, 25 mg/kg
Administration:
Result:Showed 13% oral bioavailability in mice when oral dose used 25 mg/kg.
体外研究：
HPK1-IN-21 (compound 25) (0.001, 0.01, 0.1, 1, 10, 100 μM; 4 hours) inhibits the activity of HPK1 kinase.
产品资料
Copyright©2015-2024 沪ICP备2022026524号-1
沪公网安备