AS-252424

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Chemical Structure| 900515-16-4 同义名 : -
CAS号 : 900515-16-4
货号 : A942298
分子式 : C14H8FNO4S
纯度 : 99%
分子量 : 305.28
MDL号 : MFCD12024675
存储条件：

Pure form Inert atmosphere, 2-8°C

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

DMSO: 25 mg/mL(81.89 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, IC50:33 nM

  • p110α

    PI3Kα, IC50:935 nM
描述 AS-252424 is a potent PI3Kγ inhibitor with IC50 of 30 nM in a cell-free assay with 30-fold selectivity for PI3Kγ than PI3Kα, and low inhibitory activity towards PI3Kδ/β.
细胞研究
细胞系 浓度 检测类型 检测时间 活性说明 数据源
mouse Raw264 macrophage Function assay Inhibition of C5a-mediated PKB/Akt phosphorylation in mouse Raw264 macrophage, IC50=0.23 μM 16789742
THP1 cells Function assay Inhibition of MCP1-induced PKB/Akt phosphorylation in THP1 cells, IC50=0.4 μM 16789742
实验方案
1mg 5mg 10mg

1 mM

5 mM

10 mM

3.28mL

0.66mL

0.33mL

16.38mL

3.28mL

1.64mL

32.76mL

6.55mL

3.28mL
参考文献

[1]Graves BM, Simerly T, et al. Phosphoinositide-3-kinase/akt - dependent signaling is required for maintenance of [Ca(2+)] (i), I(Ca), and Ca(2+) transients in HL-1 cardiomyocytes. J Biomed Sci. 2012 Jun 20;19:59.

[2]Pomel V, Klicic J, et al. Furan-2-ylmethylene thiazolidinediones as novel, potent, and selective inhibitors of phosphoinositide 3-kinase gamma. J Med Chem. 2006 Jun 29;49(13):3857-71.