AMG 511

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AMG 511  纯度: 98.81%

AMG 511 是一个高效、口服有效的 I 类 pan-PI3K 抑制剂,对 PI3Kα, 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。

AMG 511

AMG 511 Chemical Structure

CAS No. : 1253573-53-3

规格 价格 是否有货 数量
10 mM * 1 mL in DMSO ￥2510 In-stock
5 mg ￥2200 In-stock
10 mg ￥4200 In-stock
25 mg ￥9400 In-stock
50 mg   询价  
100 mg   询价  

* Please select Quantity before adding items.

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生物活性

AMG 511 is a potent and orally available pan inhibitor of class I PI3Ks, with Kis 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[1].

IC50 & Target

PI3Kα

4 nM (Ki)

PI3Kβ

6 nM (Ki)

PI3Kδ

2 nM (Ki)

PI3Kγ

1 nM (Ki)

体外研究
(In Vitro)

AMG 511 shows the inhibition of AKT (Ser473) phosphorylation in U87 malignant glioma (MG) cells with an IC50 of 4 nM[1].

上海金畔生物科技有限公司 has not independently confirmed the accuracy of these methods. They are for reference only.
体内研究
(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)[1].
AMG 511 shows excellent in vivo efficacy and pharmacokinetic profile[1].

上海金畔生物科技有限公司 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[1]
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[1]
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).

分子量

517.58

Formula

C22H28FN9O3S
CAS 号

1253573-53-3
运输条件

Room temperature in continental US; may vary elsewhere.
储存方式
Powder -20°C 3 years
4°C 2 years
In solvent -80°C 6 months
-20°C 1 month
溶解性数据
In Vitro: 

DMSO : 33.33 mg/mL (64.40 mM; Need ultrasonic)

配制储备液
浓度 溶剂体积 质量 1 mg 5 mg 10 mg
1 mM 1.9321 mL 9.6603 mL 19.3207 mL
5 mM 0.3864 mL 1.9321 mL 3.8641 mL
10 mM 0.1932 mL 0.9660 mL 1.9321 mL

*

请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液；一旦配成溶液，请分装保存，避免反复冻融造成的产品失效。
储备液的保存方式和期限：-80°C, 6 months; -20°C, 1 month。-80°C 储存时，请在 6 个月内使用，-20°C 储存时，请在 1 个月内使用。

In Vivo:

请根据您的实验动物和给药方式选择适当的溶解方案。以下溶解方案都请先按照 In Vitro 方式配制澄清的储备液，再依次添加助溶剂：

——为保证实验结果的可靠性，澄清的储备液可以根据储存条件，适当保存；体内实验的工作液，建议您现用现配，当天使用； 以下溶剂前显示的百
分比是指该溶剂在您配制终溶液中的体积占比；如在配制过程中出现沉淀、析出现象，可以通过加热和/或超声的方式助溶

  • 1.

    请依序添加每种溶剂： 10% DMSO    90% (20% SBE-β-CD in saline)

    Solubility: 2 mg/mL (3.86 mM); Suspended solution; Need ultrasonic

    此方案可获得 2 mg/mL (3.86 mM) 的均匀悬浊液，悬浊液可用于口服和腹腔注射。

    以 1 mL 工作液为例，取 100 μL 20.0 mg/mL 的澄清 DMSO 储备液加到 900 μL 20% 的 SBE-β-CD 生理盐水水溶液中，混合均匀。

    将 2 g 磺丁基醚 β-环糊精加入 5 mL 生理盐水中，再用生理盐水定容至 10 mL，完全溶解，澄清透明
*以上所有助溶剂都可在 上海金畔生物科技有限公司 网站选购。
参考文献

  • [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.

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