HPK1-IN-21

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HPK1-IN-21

本产品不向个人销售，仅用作科学研究，不用于任何人体实验及非科研性质的动物实验。

包装与价格：

包装	价格(元)
100mg	电议
250mg	电议
500mg	电议

产品介绍

HPK1-IN-21 是一种有效的HPK1激酶抑制剂 (Ki=0.8 nM)，HPK1-IN-21 也具有口服活性。

生物活性

HPK1-IN-21 is a potent inhibitor ofHPK1kinase inhibitor (Ki=0.8 nM), HPK1-IN-21 also has orally active^[1].

IC₅₀& Target

HPK1

0.8 nM (Ki)

体外研究
(In Vitro)

HPK1-IN-21 (compound 25; 0.001, 0.01, 0.1, 1, 10, 100 μM, 4 hours) inhibits the activity of HPK1 kinase^[1].

Cell Viability Assay^[1]

Cell Line:	human pan T cells
Concentration:	0.001, 0.01, 0.1, 1, 10, 100 μM
Incubation Time:	4 hours
Result:	Resulted in the inhibition of HPK1 kinase activity

体内研究
(In Vivo)

HPK1-IN-21 (1, 25 mg/kg) shows 13% oral bioavailability in mouse when oral dose used 25 mg/kg^[1].Pharmacokinetic Parameters of HPK1-IN-21 in mice
^[1]

compd	LM H/R/M^a,d	Hep H/R/M^b,d	mouse iv CL,V_ss^c	mouse F%^c
25	6.9/8.7/38	9.5/18/33	57,1.9	13%

^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)^[1]
Animal Model: Six female (6-9 weeks) C57BL/6 mice, 15-25 g^[1]
Dosage: 1, 25 mg/kg
Administration:
Result: Showed 13% oral bioavailability in mice when oral dose used 25 mg/kg.

分子量

445.92

Formula

C₂₂H₂₅ClFN₅O₂

运输条件

Room temperature in continental US; may vary elsewhere.

储存方式

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