HPK1-IN-68
HPK1-IN-68 (Compound 39) is a HPK1 inhibitor with an IC50 of 2.8 nM. HPK1-IN-68 blocks HPK1 signaling, inhibits HPK1-mediated phosphorylation of SLP76, and promotes the production of the IL-2 cytokine. HPK1-IN-68 antagonizes the immunosuppressive effect mediated by PGE2. HPK1-IN-68 enhances the infiltration of CD3+/CD8+ T cells into tumor tissues. HPK1-IN-68 exerts T cell-dependent antitumor efficacy in a mouse colon cancer model. HPK1-IN-68 exhibits significant synergistic antitumor effects when used in combination with anti-PD-1. HPK1-IN-68 is applicable to research related to colon cancer.
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- CAS. Nr.: 3078477-58-1
- Formel: C23H28FN7O2
- Molecular Weight:453.51
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Speicherung:
Please store the product under the recommended conditions in the Certificate of Analysis.
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Biologische Aktivität
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Chemical Information
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Biologische Aktivität
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HPK1 2.8 nM (IC50) |
IL-2 |
HPK1-IN-68 (pre-equilibrated for 10 min, 1 h) potently inhibits the kinase activity of recombinant HPK1, with an IC50 of 2.8 nM[1].
HPK1-IN-68 (0-1000 nM; 2 h) inhibits HPK1-mediated phosphorylation of SLP76 in Jurkat T cells, with an IC50 of 30.4 nM[1].
HPK1-IN-68 (0.01 nM-1 μM; 48 h) enhances IL-2 cytokine production in CD3/CD28-stimulated Jurkat T cells at submicromolar concentrations[1].
HPK1-IN-68 exhibits moderate metabolic stability in liver microsomes, with a half-life of 26.1 min[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:Jurkat T cells
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Concentration:0.01 nM-1 μM
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Incubation Time:48 h
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Result:Increased IL-2 production relative to vehicle control at concentrations from 0.01 nM to 100 nM.
Reduced IL-2 production at the highest tested concentration (1 μM).
| Species | Dose | Route | T1/2 | Vdss | AUC0-t | AUC0-∞ | CL | MRT0-∞ | Tmax | Cmax | CL/F | Vz/F | Bioavailability |
|---|---|---|---|---|---|---|---|---|---|---|---|---|---|
| Mice[1] | 1 mg/kg | i.v. | 4.8 ± 1.1 h | 16.8 ± 4.0 L/kg | 260.5 ± 20.9 ng·h/mL | 271.3 ± 21.9 ng·h/mL | 61.7 ± 5.1 mL/h/kg | 4.6 ± 1.1 h | / | / | / | / | / |
| Mice[1] | 10 mg/kg | p.o. | 4.2 ± 0.6 h | / | 743.4 ± 224.1 ng·h/mL | 755.8 ± 223.7 ng·h/mL | / | 4.5 ± 0.2 h | 1.7 ± 0.6 h | 140.1 ± 42.3 ng/mL | 235.7 ± 77.9 mL/min/kg | 89.3 ± 42.5 L/kg | 28.5 ± 8.6 % |
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:Balb/c (female, 4-5 weeks old, 18-22 g, subcutaneously injected with 5×105 CT26 tumor cells)[1]
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Dosage:10 mg/kg (monotherapy; combination with anti-PD-1)
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Administration:i.p.; bid; 17 days (monotherapy); i.p.; bid (combination with anti-PD-1, anti-PD-1 administered on days 0, 3, 7, and 10 at 5 mg/kg i.p.)
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Result:Achieved 48% tumor growth inhibition (TGI) as monotherapy.
Achieved 59% TGI with combination index (CI) < 1 and synergy score (SS) > 0 when combined with anti-PD-1 antibody, confirming synergistic activity.
Was well-tolerated, with no significant body weight loss observed.
Increased infiltration of CD3+/CD8+ T cells into tumor tissues, and this effect was amplified when combined with anti-PD-1 antibody.
Chemical Information
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CAS. Nr. 3078477-58-1
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Molecular Weight 453.51
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Formel C23H28FN7O2
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SMILES
NC1=NC=C(C2=CC(C)=C(OCCCN3CC[C@@H](F)C3)C(C)=C2)N=C1N4C=C(C(N)=O)C=N4
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Versand
Room temperature in continental US; may vary elsewhere.
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Speicherung
Please store the product under the recommended conditions in the Certificate of Analysis.
Reinheit & Dokumentation
Verweise
Calculators
Konzentration (Stammlösung) × Volumen (Stammlösung) = Konzentration (Ziellösung) × Volumen (Ziellösung)
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