| Description | AMG 511 is a potent and orally available pan inhibitor of class I PI3Ks(Kis of 4 nM, 6 nM, 2 nM and 1 nM for PI3Kα, β, δ and γ, respectively). It exhibits anti-tumor activity in mouse glioblastoma xenograft model[1]. AMG 511 significantly suppresses PI3K signaling that is indicated by p-Akt (Ser473) decrease. |
| In vitro | AMG 511 在 U87 恶性胶质瘤 (MG) 细胞中显示出对 AKT (Ser473) 磷酸化的抑制作用，其 IC50 为 4 nM[1]。 |
| In vivo | AMG 511在活体内展现出卓越的疗效及药代动力学特性[1]。在小鼠肝脏药效学模型中，AMG 511强效地阻断目标PI3K通路（3-30 mg/kg；口服）。同时，在U87 MG神经胶质瘤异种移植模型中通过口服（每天一次，连续12天；3-30 mg/kg）抑制肿瘤生长[1]。 |
| Target activity | PI3Kα:4 nM (ki), PI3Kβ:6 nM (ki), PI3Kγ:1 nM (ki), PI3Kδ:2 nM (ki) |
| molecular weight | 517.58 |
| Molecular formula | C22H28FN9O3S |
| CAS | 1253573-53-3 |
| Storage | Powder: -20°C for 3 years | In solvent: -80°C for 1 year |
| Solubility | DMSO: 33.33 mg/mL (64.40 mM), Sonication is recommended. |
| References | 1. Mark H Norman, et al. Selective Class I Phosphoinositide 3-kinase Inhibitors: Optimization of a Series of Pyridyltriazines Leading to the Identification of a Clinical Candidate, AMG 511. J Med Chem. 2012 Sep 13;55(17):7796-816. |