HPK1-IN-52 

HPK1-IN-52 is a potent and orally active hematopoietic progenitor kinase 1 (HPK1) inhibitor with an IC₅₀ value of 10.4 nM. HPK1-IN-52 exhibits anti-tumor activities^[1].

HPK1-IN-52 (compound 24) shows comparable activity (IC₅₀ of 10.4 nM) and cellular potency (pSLP76 EC₅₀ of 41 nM & IL-2 EC₅₀ of 108 nM)^[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

HPK1-IN-52 (compound 24; 30 mg/kg; po; twice daily; for two weeks) exhibits moderate tumor-growth inhibition (TGI) of 42%^[1].
HPK1-IN-52's plasma clearance significantly improved (Cl_p = 46 mL/min/kg) in mice, and its oral exposure dramatically increased (AUC_(0–24h) = 4139 h ng/mL). In addition, HPK1-IN-52 exhibits lower in vivo clearance (Cl_p = 67 mL/min/kg) and higher oral exposure (AUC_(0–24h) = 2013 h ng/mL) in rats^[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

556.61

C₃₁H₃₀F₂N₆O₂

2994298-66-5

O=C1NC=CC2=C1C(NC3=NC(CN4C[C@@H](F)CC4)=C(C5CCOCC5)C=C3)=CC=C2C6=CN=C7C=C(F)C=CN76

Room temperature in continental US; may vary elsewhere.

Please store the product under the recommended conditions in the Certificate of Analysis.

• [1]. Jingjing Peng, et al. Discovery of 1(2H)-phthalazinone and 1(2H)-isoquinolinone derivatives as potent hematopoietic progenitor kinase 1 (HPK1) inhibitors. European Journal of Medicinal Chemistry. Volume 279, 5 December 2024, 116877.