1. MAPK/ERK Pathway
    Protein Tyrosine Kinase/RTK
  2. MAP4K
    FLT3
    Src
  3. HPK1-IN-2

HPK1-IN-2 

Cat. No.: HY-132150
Handling Instructions

HPK1-IN-2 is a potent and orally active hematopoietic progenitor kinase-1 (HPK1) inhibitor (IC50<0.05 µΜ) with antitumor activity. HPK1-IN-2 also inhibits Lck (0.05 µΜ<IC50<0.5 µΜ) and Flt3 (IC50<0.05 µΜ) kinase activities.

For research use only. We do not sell to patients.

HPK1-IN-2 Chemical Structure

HPK1-IN-2 Chemical Structure

CAS No. : 2056122-11-1

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Description

HPK1-IN-2 is a potent and orally active hematopoietic progenitor kinase-1 (HPK1) inhibitor (IC50<0.05 µΜ) with antitumor activity. HPK1-IN-2 also inhibits Lck (0.05 µΜ<IC50<0.5 µΜ) and Flt3 (IC50<0.05 µΜ) kinase activities[1].

IC50 & Target

IC50: <0.05 µΜ (HPK1); <0.05 µΜ (Flt3); 0.05-0.5 µΜ (Lck)[1]

In Vitro

In a-CD3 stimulated Jurkat E6. 1 cells, HPK1-IN-2 (example A1) inhibits SLP76 serine 376 phosphorylation and ERK1/2 T202/Y204 phosphorylation with IC50 values of 0.3-1 µΜ and >3µΜ, respectively[1].

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

In Vivo

HPK1-IN-2 (example A1; 75-150 mg/kg; oral gavage; daily; for 21 days) treatment shows a dose-dependently tumor growth inhibition, with 75 mg/kg and 150 mg/kg QD inhibiting tumour growth by 44% and 64%, respectively[1].

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

Animal Model: Female BALB/c mice (6-8week old) injected with CT26 cancer cells[1]
Dosage: 75 mg/kg and 150 mg/kg
Administration: Oral gavage; daily; for 21 days
Result: Showed a dose-dependently tumor growth inhibition.
Molecular Weight

380.47

Formula

C₁₉H₂₀N₆OS

CAS No.

2056122-11-1

SMILES

O=C1C(C2=NC3=CC=C(N4CCN(C)CC4)C=C3N2)=C(N)C(C=CS5)=C5N1

Shipping

Room temperature in continental US; may vary elsewhere.

Storage

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

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Keywords:

HPK1-IN-2MAP4KFLT3SrcMAPK Kinase Kinase KinaseCluster of differentiation antigen 135CD135Fms like tyrosine kinase 3immunecheckpointHPK1antitumorSLP76serine-376Inhibitorinhibitorinhibit

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HPK1-IN-2
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HY-132150
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