2. MAPK/ERK Pathway
  3. MAP4K
  4. 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.

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HPK1-IN-21 Chemical Structure

HPK1-IN-21 Chemical Structure

CAS No. : 2413804-83-6

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HPK1-IN-21 Related Antibodies

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MAP4K2/GCK MAP4K3/GLK MAP4K4/HGK MAP4K5/KHS1 MAP4K6/MINK1 MAP4K7/TNIK MAP4K1/HPK1

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Description

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)

Cellular Effect
Cell Line Type Value Description References
T-cell EC50
1.56 μM
Compound: 25
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
[PMID: 35059127]
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].

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

HPK1-IN-21 Related Antibodies

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
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]

MedChemExpress (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.
Molecular Weight

445.92

Formula

C22H25ClFN5O2
CAS No.
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
Shipping

Room temperature in continental US; may vary elsewhere.
Storage

Please store the product under the recommended conditions in the Certificate of Analysis.
Purity & Documentation
References
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HPK1-IN-21 Related Classifications

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Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

HPK1-IN-212413804-83-6MAP4KMAPK Kinase Kinase Kinaseantitumororal bioavailabilityT cellsInhibitorinhibitorinhibit

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