AMG319|cas:1608125-21-8|西域试剂

AMG319,98.27%

产品编号：Bellancom-12948| CAS NO：1608125-21-8| 分子式：C₂₁H₁₆FN₇| 分子量：385.40

本网站销售的所有产品仅用于工业应用或者科学研究等非医疗目的,不可用于人类或动物的临床诊断或者治疗,非药用,非食用，

货号	价格	库存与货期
Bellancom-12948	￥850.00	杭州北京（现货）
Bellancom-12948	￥1400.00	杭州北京（现货）
Bellancom-12948	￥2900.00	杭州北京（现货）
Bellancom-12948	￥5000.00	杭州北京（现货）
Bellancom-12948	￥7700.00	杭州北京（现货）

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AMG319

产品介绍

AMG319 是一种有效的选择性 PI3Kδ 抑制剂，IC₅₀ 为 18 nM。

生物活性

AMG319 is a potent and selective PI3Kδ kinase inhibitor with IC₅₀ of 18 nM.

体外研究

AMG319 inhibits PI3Kδ, PI3Kγ, PI3Kβ and PI3Kα with IC₅₀s of 18 nM, 850 nM, 2.7 μM and 33 μM, respectively. AMG319, a compound with an IC₅₀ of 16 nM in a human whole blood assay (HWB), excellent selectivity over a large panel of protein kinases, and a high level of in vivo efficacy as measured by two rodent disease models of inflammation. AMG319 has minimal CYP3A4/2D6 inhibition and does not inhibit CYPs (1A2, 2C8, 2C9, 2C19, 2E1, all >20 μM). There is no time dependent inhibition (TDI) against CYPs 3A4, 2D6, 1A2, and 2C9 nor CYP induction (3A4, 2D6, 1A2, 2B6) as measured in hepatocytes. AMG319 is clean in a hERG binding assay (>25 μM), and an Ames micronucleus test proved negative. AMG319 has minimal effects in a BSEP assay up to >200 μM. Additionally, AMG319 is clean in a large side effect profiling panel (CEREP) and has no activity in a large panel of 359 unique protein kinases tested at 10 μM drug concentration.

西域 has not independently confirmed the accuracy of these methods. They are for reference only.

体内研究

The study is performed to determine the correlation between biochemical coverage (i.e., pAKT) with functional activity in vivo. AMG319 achieves this coverage at the 3 mg/kg level, which also coveres the human whole blood assay (HWB) (CD-69) IC₉₀ at trough for a full 24 h period. The lower doses 0.1, 0.3, and 1 mg/kg cover trough concentrations between the HWB IC₅₀ and IC₉₀ and evince partial efficacy. Similarly, the plasma concentration of AMG319 covers the IC₉₀ at the 1 mg/kg dose of the mouse anti-IgM pAKT in vitro assay.

西域 has not independently confirmed the accuracy of these methods. They are for reference only.

体内研究

西域 has not independently confirmed the accuracy of these methods. They are for reference only.

性状

Solid

溶解性数据

In Vitro:

DMSO : 50 mg/mL (129.74 mM; Need ultrasonic)

配制储备液

浓度溶剂体积质量	1 mg	5 mg	10 mg

1 mM	2.5947 mL	12.9735 mL	25.9471 mL
5 mM	0.5189 mL	2.5947 mL	5.1894 mL
10 mM	0.2595 mL	1.2974 mL	2.5947 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 40% PEG300 5% Tween-80 45% saline
Solubility: ≥ 2.5 mg/mL (6.49 mM); Clear solution

此方案可获得 ≥ 2.5 mg/mL (6.49 mM，饱和度未知) 的澄清溶液。
以 1 mL 工作液为例，取 100 μL 25.0 mg/mL 的澄清 DMSO 储备液加到 400 μL PEG300 中，混合均匀；向上述体系中加入50 μL Tween-80，混合均匀；然后继续加入 450 μL生理盐水定容至 1 mL。
将 0.9 g 氯化钠，完全溶解于 100 mL ddH₂O 中，得到澄清透明的生理盐水溶液
2.

请依序添加每种溶剂： 10% DMSO 90% (20% SBE-β-CD in saline)
Solubility: ≥ 2.5 mg/mL (6.49 mM); Clear solution

此方案可获得 ≥ 2.5 mg/mL (6.49 mM，饱和度未知) 的澄清溶液。
以 1 mL 工作液为例，取 100 μL 25.0 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
3.

请依序添加每种溶剂： 10% DMSO 90% corn oil
Solubility: ≥ 2.5 mg/mL (6.49 mM); Clear solution

此方案可获得 ≥ 2.5 mg/mL (6.49 mM，饱和度未知) 的澄清溶液，此方案不适用于实验周期在半个月以上的实验。
以 1 mL 工作液为例，取 100 μL 25.0 mg/mL 的澄清 DMSO 储备液加到 900 μL玉米油中，混合均匀。