HPK1-IN-40-d2
HPK1-IN-40 (compound 49) is a potent and selective HPK1 inhibitor with an IC50 of 0.9 nM. HPK1-IN-40 reinvigorates T-cell receptor (TCR) signaling, promoting T-cell function and cytokine production in T cells while having anti-cancer activity.
For research use only. We do not sell to patients.
- CAS No.: 3032624-35-1
- Formula: C24H20D2FN7O3
- Molecular Weight:477.49
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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
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Solvent & Solubility
- Purity & Documentation
- References
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Help & FAQs
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Biological Activity
HPK1-IN-40 (0.1 μM, 1 μM) improves the IL-2 secretion of Jurkat cells , leads to augmented T cell function[1].
HPK1-IN-40 (0.03 μM ~ 1 μM )inhibits the HPK1 signaling in T cells[1].
Pharmacokinetic Parameters of HPK1-IN-40 in Rats[1]
| Route | Parameter | Rat (1 mg/kg) |
| IV | T1/2(h) | 0.898 |
| AUClast(h*ng/mL) | 355 | |
| Vss(L/kg) | 2.45 | |
| Clhep (mL/min/kg) | 46.8 | |
| Route | Parameter | Rat (3 mg/kg) |
| PO | T1/2 (h) | 0.499 |
| Tmax (h) | 0.250 | |
| AUClast(h*ng/mL) | 1.91 | |
| Cmax (ng/mL) | 3.62 | |
| F% | 0.179 |
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:Jurkat, primary mouse T cells
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Concentration:0.03, 0.1, 0.3, 1 (μM)
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Incubation Time:1h
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Result:Inhibited the HPK1 signaling in T cells.
HPK1-IN-40 (25 mg/kg; i.p.; bid for 10 days) combines with anti-PD1 antibody (10 mg/kg; i.p.; bid for 10 days) shows synergistic antitumor effects, the CT26 tumor growth rate of HPK1-IN-40 combined with anti-PD1 antibody is the lowest. No significant body weight loss was observed, indicative of good tolerance of the treatment [1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:CT26 Tumor-bearing mice
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Dosage:25 mg/kg
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Administration:Twice a day by intraperitoneal injection (i.p.), bid for 7 days.
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Result:Increased IFN-γ+CD3+ T in CD3+ TIL, IFN-γ+CD8+ T in CD8+ TIL, Th1 in CD4+ TIL, CD69+CD3+ T in CD3+ TIL, CD69+CD8+ T in CD8+ TIL, CD69+CD4+ T in CD4+ TIL.
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Animal Model:CT26 Tumor-bearing mice
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Dosage:HPK1-IN-40 (25 mg/kg), anti-PD1 antibody (10 mg/kg)
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Administration:HPK1-IN-40 alone / anti-PD1 antibody alone (every 3 days), or the combination treatment, twice a day by intraperitoneal injection (i.p.) for 10 days.
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Result:Showed marginal tumor growth inhibition (TGI = 19.6%). The CT26 tumor growth rate of HPK1-IN-40 combined with anti-PD1 antibody was the lowest, then anti-PD1 alone, then HPK1-IN-40. No significant body weight loss was observed.
1. This compound can be used as a tracer
2. This compound can be used as an internal standard for quantitative analysis by NMR, GC-MS, or LC-MS.
Chemical Information
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CAS No. 3032624-35-1
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Molecular Weight 477.49
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Formula C24H20D2FN7O3
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SMILES
OC([2H])([C@@H](NC1=NC(NC2=CC(C(C)(N3)C)=C(C=C2)C3=O)=NC=C1C4=NN=CO4)C5=CC=C(C=C5)F)[2H]
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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.
Solvent & Solubility
The following protocol is derived from the literature and is for reference only. It is recommended to first try a small sample.
Please enter the basic information of animal experiments:
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Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Working solution concentration: 0.22 mg/mL
Purity & Documentation
References
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
HPK1-IN-40-d2 Related Classifications
HY-149773S Related Classifications
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