HPK1-IN-62
HPK1-IN-62 is a selective and orally active HPK-1 inhibitor with an IC50 of 1.22 nM. HPK1-IN-62 significantly improves GLK selectivity (> 665-fold) and LCK selectivity (> 1095-fold). HPK1-IN-62 enhances T-cell activation and demonstrated synergistic effects when combined with anti-mPD-1 therapy in the MC38 tumor model, inhibiting a tumor growth. HPK1-IN-62 can be used in the researchs of colon cancer and cancer immunotherapy.
For research use only. We do not sell to patients.
- Formula: C32H33N7O3
- Molecular Weight:563.65
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Storage:
Please store the product under the recommended conditions in the Certificate of Analysis.
To place orders, for customer services and technical support, please contact: MedChemExpress USA
Tel: 609-228-6898 E-mail: [email protected] [email protected]
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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 1.22 nM (IC50) |
GLK/MAP4K3 812 nM (IC50) |
GCK/MAP4K2 1336.9 nM (IC50) |
HPK1-IN-62 (Compound 2t) (0-10 μM ,5.2 h) is effective in inhibiting the phosphorylation of SLP76 in peripheral blood mononuclear cells (PBMCs) with an IC50 of 1.7 μM[1].
HPK1-IN-62 (1 μM) exhibits excellent metabolic stability in human liver microsomes[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:MC38 cells xenograft model established in female C57BL/6 mice, aged 6-7 weeks[1]
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Dosage:100 mg/kg with or without anti-mPD-1
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Administration:Oral administration (p.o.), twice daily for 14 days
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Result:Did not show significant tumor-suppressive effects as monotherapy. Enhanced T-cell activation and demonstrated synergistic effects when combined with anti-mPD-1, achieving a tumor growth inhibition (TGI) rate of 76%, compared to 70% with anti-mPD-1 monotherapy.
Chemical Information
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Molecular Weight 563.65
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Formula C32H33N7O3
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SMILES
N#CC1=C2C=C(NC3=NC(N[C@@H](C4=C(OCCCC2)C=CC=C4)CO)=C(C=N3)C5=CC(N6CC[C@H](C6)O)=NC=C5)C=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)
HPK1-IN-62 Related Classifications
HY-178097 Related Classifications
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