| Bioactivity | 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[1]. |
| Target | HPK1IC50: 0.9 nM |
| Invitro | HPK1-IN-40 (0.1 μM, 1 μM) 促进Jurkat细胞的IL-2分泌且抑制T细胞中的HPK1信号转导，进而增强T细胞功能[1]。HPK1-IN-40 (0.03 μM ~ 1 μM ) 抑制T细胞中HPK1信号通路[1]。1.19HPK1-IN-40在大鼠体内的药动学参数[1]Route |
| In Vivo | HPK1-IN-40单独 (25 mg/kg; i.p.; bid for 7 days) 导致CT26荷瘤小鼠体内T细胞激活，产生免疫调节[1]。HPK1-IN-40 (25 mg/kg; i.p.; bid for 10 days) 联合抗PD1抗体 (10 mg/kg; i.p.; bid for 10 days) 表现出协同抗肿瘤作用，HPK1-IN-40联合抗pd1抗体组CT26肿瘤生长幅度最低，没有观察到明显的体重减轻，表明治疗耐受性良好[1]。 Animal Model: |
| Name | HPK1-IN-40-d2 |
| Formula | C24H20D2FN7O3 |
| Molar Mass | 477.49 |
| 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]. Jing Ai, et al. Design, Synthesis, and Pharmacological Evaluation of Isoindoline Analogues as New HPK1 Inhibitors. Journal of Medicinal Chemistry. 2023，Article ASAP. |