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HPK1-IN-52 is an effective orally active hematopoietic progenitor kinase 1 (HPK1) inhibitor, displaying anti-tumor activity with an IC50 value of 10.4 nM.

| Pack Size | Price | USA Warehouse | Global Warehouse | Quantity |
|---|---|---|---|---|
| 25 mg | Inquiry | 3-6 months | 3-6 months | |
| 50 mg | Inquiry | 3-6 months | 3-6 months | |
| 100 mg | Inquiry | 3-6 months | 3-6 months |
| Description | HPK1-IN-52 is an effective orally active hematopoietic progenitor kinase 1 (HPK1) inhibitor, displaying anti-tumor activity with an IC50 value of 10.4 nM. |
| Targets&IC50 | MAP4K5:104 nM, MAP4K2:448 nM, HPK1:10.4 nM, MAP4K4:665 nM, MAP4K6:168 nM, GLK/MAP4K3:85 nM |
| In vitro | HPK1-IN-52 (compound 24) exhibits significant activity (IC 50 of 10.4 nM) and cellular potency (pSLP76 EC 50 of 41 nM and IL-2 EC 50 of 108 nM). |
| In vivo | HPK1-IN-52 (compound 24; 30 mg/kg; oral administration; twice daily; for two weeks) demonstrated moderate tumor growth inhibition (TGI) with a TGI of 42%. In mice, HPK1-IN-52 showed significantly increased plasma clearance (Clp = 46 mL/min/kg) and significantly higher oral exposure (AUC (0–24h) = 4139 h ng/mL). Additionally, in rats, this compound exhibited a lower in vivo clearance rate (Clp = 67 mL/min/kg) and higher oral exposure (AUC (0–24h) = 2013 h ng/mL). |
| Molecular Weight | 556.61 |
| Formula | C31H30F2N6O2 |
| Cas No. | 2994298-66-5 |
| Smiles | N(C1=C2C(=C(C=C1)C=3N4C(=NC3)C=C(F)C=C4)C=CNC2=O)C=5N=C(CN6C[C@@H](F)CC6)C(=CC5)C7CCOCC7 |
| Storage | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice/Shipping at ambient temperature. |
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.
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.
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