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- 详细信息
- 文献和实验
- 技术资料
- 保存条件：
Powder: -20°C, 3 years; 4°C, 2 years. In solvent: -80°C, 6 months; -20°C, 1 month.
- 库存：
货期：1-2天
- 供应商：
MedChemExpress LLC
- CAS号：
1608125-21-8
- 规格：
10 mM * 1 mL/5 mg/10 mg/25 mg/50 mg/100 mg
| 规格： | 10 mM * 1 mL | 产品价格： | ￥930.0 |
|---|---|---|---|
| 规格： | 5 mg | 产品价格： | ￥850.0 |
| 规格： | 10 mg | 产品价格： | ￥1400.0 |
| 规格： | 25 mg | 产品价格： | ￥2900.0 |
| 规格： | 50 mg | 产品价格： | ￥5000.0 |
| 规格： | 100 mg | 产品价格： | ￥7700.0 |
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AMG319
CAS No. : 1608125-21-8
MCE 国际站：AMG319
产品活性：AMG319 是一种有效的选择性 PI3Kδ 抑制剂，IC50 为 18 nM。
研究领域：PI3K/Akt/mTOR
作用靶点：PI3K
In Vitro: 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.
In Vivo: 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.
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文献和实验Silver Acetate Autometallography (AMG)
In the early eighties, a series of papers were published by Gorm DANSCHER, Aarhus, Denmark, to introduce a reliable and easy-to-handle technique for light microscopical and ultrastructural autometallographic (AMG) studies. Specific methods
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