AMG-511-DataSheet-生命科学试剂-MedChemExpress.pdf免费

Hotline: 400-820-3792 Inhibitors • Agonists • Screening Libraries www.MedChemE AMG 511 Cat. No.: HY-13440 CAS No.: 1253573-53-3 分⼦式: C₂₂H₂₈FN₉O₃S 分⼦量: 517.58 作⽤靶点: PI3K 作⽤通路: PI3K/Akt/mTOR 储存⽅式: Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month BIOLOGICAL ACTIVITY ⽣物活性 AMG 511 是⼀个⾼效、⼝服有效的 I 类 pan-PI3K 抑制剂,对 PI3K α, β, δ 和 γ 作⽤的 Ki 值分别为 4 nM, 6 nM, 2 nM 和 1 nM。AMG 511 减少 p-Akt (Ser473), 体现了它显著抑制了 PI3K 信号。AMG 511 在⼩⿏胶质母细 胞瘤移植瘤模型中具有抗肿瘤活性 [1]。 IC50 Target PI3Kα PI3Kβ PI3Kδ PI3Kγ 4 nM (Ki) 6 nM (Ki) 2 nM (Ki) 1 nM (Ki) 体外研究 AMG 511 shows the inhibition of AKT (Ser473) phosphorylation in U87 malignant glioma (MG) cells with an IC50 of 4 nM [1]. 体内研究 AMG 511 potently blocks the targeted PI3K pathway in a mouse liver pharmacodynamic model (3-30 mg/kg; p.o.) and inhibits tumor growth in a U87 MG glioblastoma xenograft model (3-30 mg/kg; p.o.; daily; for 12 days) [1]. AMG 511 shows excellent in vivo efficacy and pharmacokinetic profile [1]. Animal Model: Female CD1 NU/NU mice, with U87 MG glioblastoma