| Description | IHMT-PI3K-455 (Compound 15u) is a potent, selective PI3Kγ/δ dual inhibitor, demonstrating oral activity, with IC50 values of 7.1 nM for PI3Kγ and 0.57 nM for PI3Kδ. This compound inhibits AKT phosphorylation and promotes tumor regression through the recruitment and activation of CD8+ T cells. It is utilized in cancer research [1]. |
| In vitro | IHMT-PI3K-455（1μM，2小时）在RAW264.7和Raji细胞中抑制PI3Kγ/δ介导的AKT磷酸化[1]。同一化合物（1μM，72小时）影响THP-1与BMDM衍生M2型巨噬细胞的极化[1]。 |
| In vivo | IHMT-PI3K-455 (40 mg/kg，口服；每日一次，连续30天) 显著抑制了MC38肿瘤异种移植模型的肿瘤生长 [1]。该化合物通过促进CD8+ 杀伤性T细胞的招募与激活达到抑瘤作用 [1]。在Sprague-Dawley 大鼠体内，IHMT-PI3K-455 的药代动力学参数如下 [1]：剂量(mg/kg) 途径 Cmax (ng/mL) Tmax (h) AUC0-∞ (h⋅ng/mL) T1/2 (h) CL (L/h/kg) Vz (L/kg) F (%) 1 i.v. 1233 0.03 477 1.59 2.12 4.80 – 10 p.o. 157 3.42 838 2.71 14.76 56.02 17.6。 |
| Target activity | PI3Kα:6.717 μM, PI3Kβ:42.04 nM, PI3Kγ:7.1 nM, PI3Kδ:0.57 nM |
| molecular weight | 517.49 |
| Molecular formula | C26H21F2N7O3 |
| Storage | Powder: -20°C for 3 years | In solvent: -80°C for 1 year |