HPK1-IN-21
HPK1-IN-21 is a potent inhibitor of HPK1 kinase inhibitor (Ki=0.8 nM). HPK1-IN-21 also has orally active.
For research use only. We do not sell to patients.
- CAS No.: 2413804-83-6
- Formula: C22H25ClFN5O2
- Molecular Weight:445.92
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Storage:
Please store the product under the recommended conditions in the Certificate of Analysis.
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Biological Activity
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Chemical Information
- Purity & Documentation
- References
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Biological Activity
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HPK1 0.8 nM (Ki) |
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Cell Line
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Type | Value | Description | References |
|---|---|---|---|---|
| T-cell | EC50 |
1.56 μM
Compound: 25
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Effects of compound on IL-2 production in human pan T-cells followed by anti-CD3/CD28-stimulation assessed as increase in IL-2 level incubated for 30 mins by ELISA method
Effects of compound on IL-2 production in human pan T-cells followed by anti-CD3/CD28-stimulation assessed as increase in IL-2 level incubated for 30 mins by ELISA method
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[PMID: 35059127] |
HPK1-IN-21 (compound 25) (0.001, 0.01, 0.1, 1, 10, 100 μM; 4 hours) inhibits the activity of HPK1 kinase[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:human pan T cells
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Concentration:0.001, 0.01, 0.1, 1, 10, 100 μM
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Incubation Time:4 hours
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Result:Resulted in the inhibition of HPK1 kinase activity
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]
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:Six female (6-9 weeks) C57BL/6 mice, 15-25 g[1]
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Dosage:1, 25 mg/kg
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Administration:
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Result:Showed 13% oral bioavailability in mice when oral dose used 25 mg/kg.
Chemical Information
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CAS No. 2413804-83-6
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Molecular Weight 445.92
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Formula C22H25ClFN5O2
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SMILES
CN(C(C1=C(C(C2=C(C3=C(NC[C@@]34CC[C@](C(N)=O)(C4)C)N=C2)Cl)=CC=C1N)F)=O)C
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Shipping
Room temperature in continental US; may vary elsewhere.
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Storage
Please store the product under the recommended conditions in the Certificate of Analysis.
Purity & Documentation
References
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
HPK1-IN-21 Related Classifications
HY-144073 Related Classifications
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