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AMG319

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Chemical Structure| 1608125-21-8 同义名 : -
CAS号 : 1608125-21-8
货号 : A243115
分子式 : C21H16FN7
纯度 : 99%
分子量 : 385.397
MDL号 : MFCD28902228
存储条件：

粉末 Keep in dark place,Sealed in dry,Store in freezer, under -20°C

液体 -20°C:3-6个月-80°C:12个月
溶解度 :

DMSO: 50 mg/mL(129.74 mM)，配合低频超声助溶，注意：DMSO长时间开封后，会吸水并导致溶解能力下降，请避免使用长期开封的DMSO
动物实验配方：
生物活性
靶点

  • p110γ

    PI3Kγ, IC50:850 nM

  • p110δ

    PI3Kδ, IC50:18 nM
描述 AMG319 exhibits inhibitory activity against PI3Kδ, PI3Kγ, PI3Kβ, and PI3Kα with IC50 values of 18 nM, 850 nM, 2.7 μM, and 33 μM, respectively. In a human whole blood assay (HWB), AMG319 demonstrates an IC50 of 16 nM, exceptional selectivity across a broad range of protein kinases, and high efficacy in vivo as demonstrated in two rodent models of inflammation. Additionally, AMG319 shows minimal inhibition of CYP3A4/2D6 and lacks inhibitory effects on CYPs (1A2, 2C8, 2C9, 2C19, 2E1, all >20 μM). It does not exhibit time-dependent inhibition (TDI) or induction against CYPs 3A4, 2D6, 1A2, 2C9, 2B6 as assessed in hepatocytes. AMG319 demonstrates negligible binding to hERG (>25 μM) and yields negative results in an Ames micronucleus test. Furthermore, AMG319 exhibits minimal impact in a BSEP assay up to >200 μM [1].
实验方案
1mg 5mg 10mg

1 mM

5 mM

10 mM

2.59mL

0.52mL

0.26mL

12.97mL

2.59mL

1.30mL

25.95mL

5.19mL

2.59mL
参考文献

[1]Cushing TD, et al. Discovery and in vivo evaluation of (S)-N-(1-(7-fluoro-2-(pyridin-2-yl)quinolin-3-yl)ethyl)-9H-purin-6-amine (AMG319) and related PI3Kδ inhibitors for inflammation and autoimmune disease. J Med Chem. 2015 Jan 8;58(1):480-511.