| Bioactivity | IHMT-PI3K-455 (Compound 15u) is a potent, selective, orally active PI3Kγ/δ dual inhibitor with IC50s of 7.1 nM and 0.57 nM for PI3Kγ and PI3Kδ, respectively. IHMT-PI3K-455 suppresses the AKT phosphorylation. IHMT-PI3K-455 inhibits tumor growth by recruiting and activating more CD8+ killing T cells.IHMT-PI3K-455 is used in cancer research[1]. |
| Invitro | IHMT-PI3K-455 (1 μM，2 小时) 抑制了 RAW264.7 和 Raji 细胞中 PI3Kγ/δ 介导的 AKT 磷酸化[1]。IHMT-PI3K-455 (1 μM，72 小时) 改变由 THP-1 和 BMDM 细胞衍生的 M2 巨噬细胞的极化[1]。 0 --> IHMT-PI3K-455 相关抗体: Cell Differentiation Assay[1] Cell Line: |
| In Vivo | IHMT-PI3K-455 (40 mg/kg，口服；一天一次，连用 30 天) 抑制了 MC38 肿瘤异种移植模型中的肿瘤生长[1]。IHMT-PI3K-455 (40 mg/kg，口服；一天一次，连用 30 天) 通过招募和激活更多 CD8+ 杀伤 T 细胞抑制肿瘤生长[1]。Pharmacokinetic parameters of IHMT-PI3K-455 in Sprague-Dawley rats[1]Dose (mg/kg) |
| Name | IHMT-PI3K-455 |
| Formula | C26H21F2N7O3 |
| Molar Mass | 517.49 |
| 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]. Liang X, et al. Discovery of Pyrazolo[1,5-a]pyrimidine derivative as a potent and selective PI3Kγ/δ dual inhibitor. Eur J Med Chem. 2023 Nov 15;260:115768. |