HPK1-IN-21

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HPK1-IN-21;

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。

HPK1-IN-21amp;;

HPK1-IN-21 Chemical Structure

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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[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].

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

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/Ma,d Hep H/R/Mb,d mouse iv CL,Vssc 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]

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

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.
参考文献

  • [1]. Discovery of Spiro-azaindoline Inhibitors of Hematopoietic Progenitor Kinase 1 (HPK1). ACS Med Chem Lett. 2021, 13(1):84-91.