AMG 511
规格
| Cas Number | 1253573-53-3 |
| 规格或纯度 | ≥99% |
| 纯度 | ≥99% |
| 包装 | 10mg 或 1mg 或 5mg 或 25mg |
产品信息
| 品牌 | 阿拉丁 |
| 溶解性 | DMSO : 33.33 mg/mL (64.40 mM; Need ultrasonic) |
| 过滤标签 | PI3K,PI3K/Akt/mTOR |
| 储存温度 | -20°C储存 |
| 运输条件 | 超低温冰袋运输 |
| 生化和生理学机理 | AMG 511 是一种强效的口服 I 类 PI3K 泛抑制剂，对 PI3Kα 、β、δ 和γ 的 K i s 分别为 4 nM、6 nM、2 nM 和 1 nM。AMG 511 能明显抑制 PI3K 信号转导，p-Akt（Ser473）的下降表明了这一点。AMG 511 e |
| 英文描述 |
AMG 511 is a potent and orally available pan inhibitor of class I PI3K s, with K i s of 4 nM, 6 nM, 2 nM and 1 nM for PI3Kα , β, δ and γ, respectively. AMG 511 significantly suppresses PI3K signaling that is indicated by p-Akt (Ser473) decrease. AMG 511 exhibits anti-tumor activity in mouse glioblastoma xenograft model In Vitro AMG 511 shows the inhibition of AKT (Ser473) phosphorylation in U87 malignant glioma (MG) cells with an IC 50 of 4 nM. MCE has not independently confirmed the accuracy of these methods. They are for reference only. In Vivo 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) . AMG 511 shows excellent in vivo efficacy and pharmacokinetic profile . MCE has not independently confirmed the accuracy of these methods. They are for reference only. Animal Model: Female CD1 NU/NU mice, with U87 MG glioblastoma xenograft model Dosage: 1 mg/kg, 3 mg/kg, 10 mg/kg Administration: Oral administration, daily, for 12 days Result: Inhibited tumor growth. Animal Model: Male Sprague-Dawley rats Dosage: 1 mg/kg Administration: Oral administration (Pharmacokinetic Analysis) Result: Had a superior pharmacokinetic profile with low clearance (0.4 L/h/kg, 12% of liver blood flow), good oral bioavailability (F = 60%), and a commensurate high oral exposure (AUC = 5.0 μM·h). Form:Solid IC50& Target:PI3Kα 4 nM (Ki) PI3Kβ 6 nM (Ki) PI3Kδ 2 nM (Ki) PI3Kγ 1 nM (Ki) |