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AS-604850

AS604850 是一种有效的，选择性的、和 ATP 竞争性的PI3Kγ抑制剂，其 IC50=0.25 μM，Ki=0.18 μM。它是一种PI3Kγ的同工型选择性抑制剂，对PI3Kγ的选择性是 PI3Kδ/β 的 30 倍以上，是 PI3Kα 的 18 倍以上。

CAS号

648449-76-7

分子式

C11H5F2NO4S

主要靶点

PI3K

仅限科研使用

Cat No : CM05936

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Synonyms

5-[(2,2-二氟-1,3-苯并二恶茂-5-基)亚甲基]噻唑烷-2,4-二酮

验证数据展示

  • CAS No.: 648449-76-7

    AS-604850
    CAS#: 648449-76-7

产品信息

AS-604850 is a specific and ATP-competitive PI3Kγ inhibitor (IC50: 250 nM), 18-fold more selective for PI3Kγ than PI3Kα, and over 80-fold selectivity for PI3Kγ than PI3Kδ/β.

CAS号 648449-76-7
分子式 C11H5F2NO4S
主要靶点 PI3K
主要通路 PI3K/Akt/mTOR信号通路
分子量 285.22
纯度 99.84%， 此纯度可做参考，具体纯度与批次有关系，可咨询客服
储存条件 Powder: -20°C for 3 years | In solvent: -80°C for 1 year
别名 5-[(2,2-二氟-1,3-苯并二恶茂-5-基)亚甲基]噻唑烷-2,4-二酮

靶点活性

PI3Kγ:250 nM

体内活性

AS-604850 reduces RANTES-induced peritoneal neutrophil recruitment with a ED50 of 42.4 mg/kg. In the thioglycollate-induced peritonitis model, oral administration of 10 mg/kg AS-604850 results in a 31% reduction of neutrophil recruitment. [1]

体外活性

AS-604850 is ATP-competitive PI3Kγ inhibitor with Ki values of 0.18 μM. AS-604850 is isoform selective inhibitor of PI3Kγ with over 30-fold selectivity for PI3Kδ and β, and 18-fold selectivity over PI3Kα. (PI3Kα: IC50 = 4.5 μM, PI3Kγ and β: IC50 > 20 μM) AS-604850 is capable of inhibiting C5a-mediated PKB phosphorylation in RAW264 mouse macrophages with an IC50 with 10 μM. AS-604850 blocks MCP-1-mediated chemotaxis in Pik3cg +/+ monocytes in a concentration- dependent manner, with an IC50 of 21 mM, but dosn't affect chemotaxis in Pik3cg-/- cells, indicating that AS-604850 acts through PI3Kγ. [1] AS-604850 diminishes glycochenodeoxycholate (GCDC) induced Akt-phosphorylation and apoptosis in rat hepatocytes. AS-604850 diminishes bile salt-induced apoptosis in HepG2 Ntcp and Huh7-Ntcp cells. [2] AS604850 causes a concentration-dependent suppression of chemotactic responses of EoL-1 cells and blood eosinophils to platelet-activating factor (PAF). [3]

溶解度

Ethanol:5 mg/mL (17.53 mM),H2O:<1 mg/mL,DMSO:57 mg/mL (199.84 mM)

细胞实验

Hepatocyte cultures are treated with diluent (DMSO), 25 μM TLC, 250 μM TCDC, 50 μM GCDC, or 50 ng/ml Fas for 2-4 hours HepG2-Ntcp and Huh7-Ntcp cells are treated with DMSO, 20 μM TLC, 75 μM TCDC or GCDC, 200 μM etoposide or 200 ng/ml TNFa plus 28 ng/ml actinomycin D for 2-4 hours. The number of apoptotic cells is determined morphologically using fluorescent staining and expressed as % of cells. Apoptosis is confirmed in human cell lines by determination of caspase-3/-7 activity and in rat hepatocytes by detection of the 17 kDa proteolytic cleavage fragment of caspase-3 by immunoblotting; equal protein loading is monitored by immunoblotting for actin.(Only for Reference)

参考文献

1.Camps M, et al, Nat Med, 2005, 11(9), 936-943.
2.Hohenester S, et al, J Hepatol, 2010, 53(5), 918-926.
3.Hasan AM, et al, Int Immunopharmacol, 2010, 10(9), 12017-1021.

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