AS-605240

    98%

(Z)-5-(quinoxalin-6-ylmethylene)thiazolidine-2,4-dione

源叶(MedMol)
S80862
648450-29-7
C12H7N3O2S
257.27
MFCD11100415
品牌 货号 产品规格 价格(RMB) 库存(上海) 北京 武汉 南京 购买数量
源叶(MedMol) S80862-5mg 98% ¥272.00元 10 - - -
源叶(MedMol) S80862-10mg 98% ¥493.00元 10 - - -
源叶(MedMol) S80862-50mg 98% ¥1360.00元 6 - - -
源叶(MedMol) S80862-100mg 98% ¥2295.00元 5 - - -
产品介绍 参考文献 质检证书(COA) 摩尔浓度计算器 相关产品

产品介绍

AS-605240 is a specific and orally active inhibitor of the PI3Kγ, with an IC50 of 8 nM, and a Ki of 7.8 nM.
产品描述: AS-605240 is a specific and orally active inhibitor of the PI3Kγ, with an IC50 of 8 nM, and a Ki of 7.8 nM.
靶点: PI3Kα:60 nM (IC50);PI3Kβ:270 nM (IC50);PI3Kδ:300 nM (IC50);PI3Kγ:8 nM (IC50);PI3Kγ:7.8 nM (Ki);Autophagy;PI3K;Autophagy
体内研究: AS-605240 (30 mg/kg BW, per os, every 12 h) markedly decreases FoxM1 expression in mouse lungs and fails to restore vascular integrity. AS-605240 reduces RANTES-induced peritoneal neutrophil recruitment, with ED50 of 9.1 mg/kg. In the CCL5 model, AS-605240 shows an ED50 value of 10 mg/kg, in correlation with the percentage of reduction of neutrophil recruitment observed in Pik3cg-/- mice. AS-605240 (50 mg/kg, p.o.) substantially reduces clinical and histological signs of joint inflammation to a similar extent to that of Pik3cg-/- mice. AS605240 (30 mg/kg, i.p.) suppresses intracellular PAkt in splenocytes of NOD mice and delays diabetes onset. AS605240 also prevents autoimmune diabetes in prediabetic NOD mice, and suppresses autoreactive T cells while increasing Tregs in NOD mice. AS605240 (30 mg/kg, i.p.) reverses hyperglycemia in newly hyperglycemic NOD mice, reverses hyperglycemia in early diabetic NOD mice through Tregs and suppresses T-cell infiltration in pancreatic islets while increasing Tregs. AS605240 (25, 50 mg/kg) markedly reduces total cell count and numbers of macrophages, neutrophils and lymphocytes in rats. AS605240 significantly reduces the levels of TNF-α and IL-1β in BALF to 132.7±11.2 pg/mL and 49.2±11.3 pg/mL in 25 mg/kg AS605240 + BLM group and 131.3±10.7 and 49.6±8.8 pg/mL in 50 mg/kg AS605240 + BLM group, respectively. AS605240 inhibits prefibrotic cytokines production in bleomycin-induced pulmonary fibrosis. AS605240 inhibits phosphorylation of Akt of inflammatory cells in b
参考文献: 1. Huang X, et al. Endothelial p110γPI3K Mediates Endothelial Regeneration and Vascular Repair After Inflammatory Vascular Injury. Circulation. 2016 Mar 15;133(11):1093-103. 2. Camps M, et al. Blockade of PI3Kgamma suppresses joint inflammation and damage in mouse models of rheumatoid arthritis. Nat Med. 2005 Sep;11(9):936-43. 3. Azzi J, et al. The novel therapeutic effect of phosphoinositide 3-kinase-γ inhibitor AS605240 in autoimmune diabetes. Diabetes. 2012 Jun;61(6):1509-18. Epub 2012 Mar 8. 4. Wei X, et al. A phosphoinositide 3-kinase-gamma inhibitor, AS605240 prevents bleomycin-induced pulmonary fibrosis in rats. Biochem Biophys Res Commun. 2010 Jun 25;397(2):311-7. Epub 2010 May 26.
溶解性: DMSO  :  3.33  mg/mL  (12.94  mM;  ultrasonic  and  warming  and  heat  to  80°C)    H2O  :  2.78  mg/mL  (10.81  mM;  ultrasonic  and  warming  and  adjust  pH  to  10  with  NaOH  and  heat  to  60°C)
保存条件: -20℃
配置溶液浓度参考:
1mg 5mg 10mg
1 mM 3.887 ml 19.435 ml 38.87 ml
5 mM 0.777 ml 3.887 ml 7.774 ml
10 mM 0.389 ml 1.943 ml 3.887 ml
50 mM 0.078 ml 0.389 ml 0.777 ml
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参考文献

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