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HPK1-IN-68
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Catalog No. T218514 Copy Product Info
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HPK1-IN-68 (Compound 39) is an HPK1 inhibitor with an IC50 of 2.8 nM. It effectively blocks HPK1 signaling, impedes HPK1-mediated SLP76 phosphorylation, and enhances IL-2 cytokine production. Additionally, HPK1-IN-68 counteracts PGE2-mediated immunosuppression and promotes infiltration of CD3+/CD8+ T cells into tumor tissue. It demonstrates T cell-dependent antitumor efficacy in a mouse colon cancer model and shows significant synergistic antitumor effects when combined with anti-PD-1 therapy. HPK1-IN-68 is applicable for research related to colon cancer.
HPK1-IN-68
Cas No. 3078477-58-1
| Pack Size | Price | USA Stock | Global Stock | Quantity |
|---|---|---|---|---|
| 10 mg | Inquiry | 10-14 weeks | 10-14 weeks | |
| 50 mg | Inquiry | 10-14 weeks | 10-14 weeks |
For In stock only · Estimated delivery: USA Stock (1-2 days) Global Stock (5-7 days)
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For research use only—not for human use. No sales to individuals. Use as intended only.
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Product Introduction
Bioactivity
Chemical Properties
Storage & Solubility Information
| Description | HPK1-IN-68 (Compound 39) is an HPK1 inhibitor with an IC50 of 2.8 nM. It effectively blocks HPK1 signaling, impedes HPK1-mediated SLP76 phosphorylation, and enhances IL-2 cytokine production. Additionally, HPK1-IN-68 counteracts PGE2-mediated immunosuppression and promotes infiltration of CD3+/CD8+ T cells into tumor tissue. It demonstrates T cell-dependent antitumor efficacy in a mouse colon cancer model and shows significant synergistic antitumor effects when combined with anti-PD-1 therapy. HPK1-IN-68 is applicable for research related to colon cancer. |
| Targets & IC50 | HPK1:2.8 nM |
| In vitro | HPK1-IN-68 effectively inhibits recombinant HPK1 kinase activity with an IC50 of 2.8 nM when pre-equilibrated for 10 minutes and assessed at 1 hour. It inhibits HPK1-mediated SLP76 phosphorylation in Jurkat T cells with an IC50 of 30.4 nM over a concentration range of 0-1000 nM for 2 hours. Moreover, HPK1-IN-68 enhances IL-2 cytokine production in CD3/CD28 stimulated Jurkat T cells at submicromolar concentrations, tested over 0.01 nM-1 μM for 48 hours. It also exhibits moderate metabolic stability in liver microsomes, with a half-life of 26.1 minutes. |
| In vivo | HPK1-IN-68, administered at 10 mg/kg via intraperitoneal injection twice daily for 17 days, demonstrates antitumor activity both as a monotherapy and in combination with anti-PD-1 antibody in a mouse CT26 colon cancer model. |
| Molecular Weight | 453.51 |
| Formula | C23H28FN7O2 |
| Cas No. | 3078477-58-1 |
| Smiles | NC=1C(=NC(=CN1)C2=CC(C)=C(OCCCN3C[C@@H](F)CC3)C(C)=C2)N4C=C(C(N)=O)C=N4 |
| Storage | Powder: -20°C for 3 years | In solvent: -80°C for 1 year Shipping with blue ice/Shipping at ambient temperature. |
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In Vivo Formulation Calculator (Clear solution)
Please enter your animal experiment information in the following box and click Calculate to obtain the stock solution preparation method and in vivo formula preparation method:
For example, if the intended dosage is 10 mg/kg for animals weighing 20 g , with a dosing volume of 100 μL per animal, and a total of 10 animals are to be administered, using a formulation of 
10% DMSO+ 40% PEG300+ 5% Tween 80+ 45% Saline/PBS/ddH2O , the resulting working solution concentration would be 2 mg/mL.Stock Solution Preparation:
Dissolve 2 mg of the compound in 100 μL DMSO to obtain a stock solution at a concentration of 20 mg/mL . If the required concentration exceeds the compound's known solubility, please contact us for technical support before proceeding.
Preparation of the In Vivo Formulation:
1) Add 100 μL of the DMSO stock solution to 400 µL PEG300 and mix thoroughly until the solution becomes clear.
2) Add 50 µL Tween 80 and mix well until fully clarified.
3) Add 450 µL Saline,PBS or ddH2O and mix thoroughly until a homogeneous solution is obtained.
This example is provided solely to demonstrate the use of the In Vivo Formulation Calculator and does not constitute a recommended formulation for any specific compound. Please select an appropriate dissolution and formulation strategy based on your experimental model and route of administration.
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Please see Inhibitor Handling Instructions for more frequently ask questions. Topics include: how to prepare stock solutions, how to store products, and cautions on cell-based assays & animal experiments, etc
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Related Tags: HPK1-IN-68 in vivo | HPK1-IN-68 in vitro | HPK1-IN-68 formula | HPK1-IN-68 molecular weight
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