1. MAPK/ERK Pathway Immunology/Inflammation
  2. MAP4K Interleukin Related
  3. HPK1-IN-64

HPK1-IN-64 is a potent, selective, and orally active HPK1 inhibitor with an IC50 value of 1.9 nM. HPK1-IN-64 exhibits selectivity exceeding 100-fold, 80-fold, 300-fold, and 350-fold against off-target kinases such as GLK, MAP4K5, TBK1, and TNIK, respectively. HPK1-IN-64 inhibits SLP76 protein phosphorylation and IL-2 secretion. HPK1-IN-64 may be used in cancer research, such as for colorectal cancer.

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

HPK1-IN-64

HPK1-IN-64 Chemical Structure

CAS No. : 3034320-17-4

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Description

HPK1-IN-64 is a potent, selective, and orally active HPK1 inhibitor with an IC50 value of 1.9 nM. HPK1-IN-64 exhibits selectivity exceeding 100-fold, 80-fold, 300-fold, and 350-fold against off-target kinases such as GLK, MAP4K5, TBK1, and TNIK, respectively. HPK1-IN-64 inhibits SLP76 protein phosphorylation and IL-2 secretion. HPK1-IN-64 may be used in cancer research, such as for colorectal cancer[1].

IC50 & Target[1]

HPK1

1.9 nM (IC50)

IL-2

 

In Vivo

HPK1-IN-64 (Compound 6) (1.5-5 mg/kg; p.o.; twice a day) inhibits tumor growth in CT26 tumor-bearing mice[1].

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

Animal Model: (CT26 tumor model)[1]
Dosage: 1.5 mg/kg, 5 mg/kg
Administration: p.o.; twice daily
Result: Inhibited tumor growth with TGI of 56% and 93%.
Molecular Weight

499.60

Formula

C29H33N5O3

CAS No.
SMILES

O=C1C(C2=C(C=C3C4=CN=C5N4CCC[C@H]5OC)C(C)(C6=CC(N7CCOCC7)=CC=C6N2)C)=C3CN1

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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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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.

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HPK1-IN-64
Cat. No.:
HY-179111
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