Bioactivity | 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]. |
Invitro | HPK1-IN-52 (compound 24) 表现出相当的活性(IC50 为 10.4 nM)和细胞效力(pSLP76 EC50 为 41 nM 和 IL-2 EC50 为 108 nM)[1]。 MCE has not independently confirmed the accuracy of these methods. They are for reference only. 0 --> HPK1-IN-52 相关抗体: |
In Vivo | HPK1-IN-52(compound 24;30 mg/kg;口服;每日两次;持续两周)表现出中等程度的肿瘤生长抑制 (TGI),为 42%[1]。HPK1-IN-52 在小鼠中的血浆清除率显著提高 (Clp = 46 mL/min/kg),其口服暴露量显著增加 (AUC(0–24h) = 4139 h ng/mL)。此外,HPK1-IN-52 在大鼠中表现出较低的体内清除率 (Clp = 67 mL/min/kg) 和较高的口服暴露量 (AUC(0–24h) = 2013 h ng/mL)[1]。 MCE has not independently confirmed the accuracy of these methods. They are for reference only. Animal Model: |
CAS | 2994298-66-5 |
Formula | C31H30F2N6O2 |
Molar Mass | 556.61 |
Transport | Room temperature in continental US; may vary elsewhere. |
Storage | Please store the product under the recommended conditions in the Certificate of Analysis. |
Reference | [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. |