CAY10505
中文名称 | CAY10505 |
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中文同义词 | (5E)-5-[[5-(4-氟苯基)-2-呋喃基]亚甲基]-2,4-噻唑烷二酮;PI3KΓ抑制剂(CAY10505);CAY10505,PI3KΓ抑制剂;(E)-5-((5-(4-氟苯基)呋喃-2-基)亚甲基)噻唑烷-2,4-二酮 |
英文名称 | CAY10505 |
英文同义词 | CAY10505;(5E)-5-[[5-(4-Fluorophenyl)-2-furanyl]methylene]-2,4-thiazolidinedione;(E)-5-((5-(4-fluorophenyl)furan-2-yl)methylene)thiazolidine-2,4-dione;CAY10505 ( 5E)-5-[[5-(4-Fluorophenyl)-2-furanyl]methylene]-2,4-thiazolidinedione;CAY10505, >=98%;2,4-Thiazolidinedione, 5-[[5-(4-fluorophenyl)-2-furanyl]methylene]-, (5E)-;CAY10505 USP/EP/BP;CAY10505 CAY-10505 |
CAS号 | 1218777-13-9 |
分子式 | C14H8FNO3S |
分子量 | 289.28 |
EINECS号 | |
相关类别 | 小分子抑制剂,天然产物;细胞生物学试剂;Akt;mTOR;PI3K;PI3K/Akt/mTOR;Inhibitors |
Mol文件 | 1218777-13-9.mol |
结构式 |
CAY10505 性质
密度 | 1.466 |
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储存条件 | Store at -20°C |
溶解度 | 不溶于乙醇;不溶于水; DMSO 中≥14.45 mg/mL |
形态 | 固体 |
酸度系数(pKa) | 7.21±0.20(Predicted) |
颜色 | 浅黄至黄色 |
PI3Kγ 30 nM (IC 50 , Neurons) |
A class IB PI3Kγ isoform inhibitor CAY10505 at 200 nM (IC 50 =30 nM) partially reduces the baicalein-induced Akt phosphorylation in neurons. The pharmacological PI3K inhibitor CAY10505 (PIK3CG) is tested on an extended panel of multiple myeloma (MM) cell lines and freshly isolated primary MM samples. MM cells are CAY10505-treated for 3 d (MM cell lines) or 5 d (primary MM cells) respectively, and survival is analysed by flow cytometry (annexin V-FITC/PI staining). Treatment of bone marrow stromal cells (BMSCs)-co-cultured primary MM samples with the PIK3CA inhibitor CAY10505 results in anti-survival effects (mean survival relative to DMSO-treated controls: CAY10505: 84±14%, tested at 10 μM).
Administration of CAY10505 (0.6 mg/kg, p.o.), Losartan (25 mg/kg, p.o.), or Atorvastatin (30 mg/kg, p.o.) significantly increases serum nitrite and (or) nitrate concentrations in hypertensive rats. Acetylcholine (ACh) and Sodium nitroprusside (SNP) produce endothelium-dependent and-independent relaxation in isolated rat aortic ring precontracted with Phenylephrine (3 μM), in a dose dependent manner. Administration of CAY10505 (0.6 mg/kg,p.o.), Losartan (25 mg/kg, p.o.), or Atorvastatin (30 mg/kg, p.o.) significantly prevents hypertension-induced attenuation of ACh-induced endothelium-dependent relaxation. Deoxycorticosterone acetate salt (DOCA, 40 mg/kg, s.c.) induced hypertension markedly attenuates acetylcholine-induced endothelium-dependent relaxation, but does not affect SNP-induced endotheliumindependent relaxation.
安全信息
更新日期 | 产品编号 | 产品名称 | CAS号 | 包装 | 价格 |
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2024/08/19 | HY-13530 | CAY10505 | 5 mg | 233元 | |
2024/08/19 | HY-13530 | CAY10505 CAY10505 | 1218777-13-9 | 10mg | 350元 |