AZD-8835

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Chemical Structure| 1620576-64-8 同义名 : -
CAS号 : 1620576-64-8
货号 : A279294
分子式 : C22H31N9O3
纯度 : 99%
分子量 : 469.54
MDL号 : MFCD28902194
存储条件：

Pure form Keep in dark place, sealed in dry, store in freezer, under -20°C

In solvent -20°C:3-6个月-80°C:12个月
溶解度 :

DMSO: 12 mg/mL(25.56 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
生物活性
靶点

  • p110γ

    PI3Kγ, IC50:90 nM

  • p110β

    PI3Kβ, IC50:431 nM

  • p110α

    PI3Kα, IC50:6.2 nM

  • p110δ

    PI3Kδ, IC50:5.7 nM
描述 AZD8835 ia a mixed inhibitor of PI3Kα and PI3Kδ with IC50 of 6.2 nM and 5.7 nM, respectively, also with selectivity against PI3Kβ (IC50=431 nM) and PI3Kγ (IC50=90 nM).
实验方案
1mg 5mg 10mg

1 mM

5 mM

10 mM

2.13mL

0.43mL

0.21mL

10.65mL

2.13mL

1.06mL

21.30mL

4.26mL

2.13mL
参考文献

[1]Hudson K, Hancox UJ, et al. Intermittent High-Dose Scheduling of AZD8835, a Novel Selective Inhibitor of PI3Kα and PI3Kδ, Demonstrates Treatment Strategies for PIK3CA-Dependent Breast Cancers. Mol Cancer Ther. 2016 May;15(5):877-89.

[2]Barlaam B, Cosulich S, et al. Discovery of 1-(4-(5-(5-amino-6-(5-tert-butyl-1,3,4-oxadiazol-2-yl)pyrazin-2-yl)-1-ethyl-1,2,4-triazol-3-yl)piperidin-1-yl)-3-hydroxypropan-1-one (AZD8835): A potent and selective inhibitor of PI3Kα and PI3Kδ for the treatment of cancers. Bioorg Med Chem Lett. 2015 Nov 15;25(22):5155-62.