HPK1-IN-65
HPK1-IN-65 is a selective and orally active HPK1 inhibitor with an IC50 value of < 5 nM. HPK1-IN-65 inhibits HPK1 kinase activity and displays 1257-fold selectivity over the MAP4K kinase family member GLK. HPK1-IN-65 exhibits an IC50 of 92.3 nM for inhibiting pSLP76 phosphorylation. HPK1-IN-65 demonstrates an EC50 of 398 nM for stimulating IL-2 production. HPK1-IN-65 inhibits TCR-induced phosphorylation of SLP76 at Ser376 in a dose-dependent manner. HPK1-IN-65 can be further utilized for colorectal cancer research.
For research use only. We do not sell to patients.
- Formula: C23H22ClFN8O2S
- Molecular Weight:528.99
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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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Help & FAQs
All MAP4K Isoforms
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Biological Activity
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HPK1 <5 nM (IC50) |
IL-2 398 nM (EC50) |
HPK1-IN-65 (compound 34) decreases pSLP76 in a dose-dependent manner in Jurkat cell line with IC50 values of 92.3 nM[1].
HPK1-IN-65 stimulates IL- 2 production with an EC50 of 398 nM and enhances the activation up to 3.59 fold[1].
HPK1-IN-65 has the anti proliferative effect in Jurkat cells[1].
HPK1-IN-65 has selectivity against MAP4K2, MAP4K3, MAP4K4, MAP4K5, MAP4K6[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:Colorectal carcinoma cell line CT-26 cells (2.5 × 105 cells, s.c.) induced female BALB/c mice (6- week-old)[1]
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Dosage:60 mg/kg
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Administration:i.g., once daily for 14 consecutive days, Anti-PD-1 monoclonal antibody (HY-P99709) (i.p., 10 mg/kg, twice a week)
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Result:Achieved a robust anti-tumor response with a TGI of 62.90%.
Caused no significant impact on animal body weight in either monotherapy or combination groups.
Delayed the tumor growth, with the tumor growth inhibi tion (TGI) reaching 41.73 % at 14 days post-treatment (without Anti-PD-1 monoclonal antibody).
Chemical Information
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Molecular Weight 528.99
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Formula C23H22ClFN8O2S
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SMILES
FC1=C(NC2=NC=C(Cl)C(NC3=C(NS(C)(=O)=O)C(N=CC=N4)=C4C=C3)=N2)C=C5C(CCN(C)C5)=C1
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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)
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