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AS-604850 Sale

(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) 目录号 : GC12080

A selective inhibitor of PI3Kγ

AS-604850 Chemical Structure

Cas No.:648449-76-7

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2mg
¥294.00
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5mg
¥494.00
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25mg
¥1,649.00
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100mg
¥4,746.00
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Sample solution is provided at 25 µL, 10mM.

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产品描述

AS-604850 is a selective and ATP-competitive PI3Kγ inhibitor (IC50= 2.5 μM), with over 30-fold selectivity for PI3Kδ and PI3Kβ, and 18-fold selectivity over PI3Kα. [1]

PI3K (phosphatidylinositol-4,5-bisphosphate 3-kinase) is a family of enzymes involved in cellular functions such as cell growth, proliferation, differentiation, motility, survival and intracellular trafficking, which in turn are involved in cancer. It plays a key role in PI3K/Akt(PKB)/mTOR pathway.

In rat hepatocytes, AS-604850 pretreatment abolished GCDC-induced phosphorylation of Akt by 50% and inhibited apoptosis by reducing GCDC/TCDC/TLC-induced caspase-3 cleavage. [2] In PI3KCG-/-monocytes and THP-1 (human monocytic cell line), AS-604850 inhibited the PKB phosphorylation activated by MCP-1, it also blocked the MCP-1-mediated chemotaxis in a concentration dependent manner. In RAW264 mouse macrophages, C5a-mediated PKB phosphorylation was inhibited by AS-604850. [1]

In the thioglycollate-induced peritonitis model that induced multiple chemokine in vivo, oral administration of 10 mg/kg AS-604850 showed a 31% decrease of neutrophil recruitment. [1]

References:
1.  Camps M, Rückle T, Ji H et al. Blockade of PI3K-gamma suppresses joint inflammation and damage in mouse models of rheumatoid arthritis. Nat Med. 2005 Sep;11(9):936-43.
2.  Hohenester S, Gates A, Wimmer R et al. Phosphatidylinositol-3-kinase p110γ contributes to bile salt-induced apoptosis in primary rat hepatocytes and human hepatoma cells. J Hepatol. 2010 Nov;53(5):918-26.

Chemical Properties

Cas No. 648449-76-7 SDF
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
化学名 5-[(2,2-difluoro-1,3-benzodioxol-5-yl)methylidene]-1,3-thiazolidine-2,4-dione
Canonical SMILES C1=CC2=C(C=C1C=C3C(=O)NC(=O)S3)OC(O2)(F)F
分子式 C11H5F2NO4S 分子量 285.22
溶解度 DMF: 20 mg/ml,DMSO: 30 mg/ml,DMSO:PBS (pH 7.2) (1:3): .5 mg/ml,Ethanol: 5 mg/ml 储存条件 Store at -20°C
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储备液的保存方式和期限:-80°C 储存时,请在 6 个月内使用,-20°C 储存时,请在 1 个月内使用。
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1 mM 3.5061 mL 17.5303 mL 35.0607 mL
5 mM 0.7012 mL 3.5061 mL 7.0121 mL
10 mM 0.3506 mL 1.753 mL 3.5061 mL
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