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1218777-13-9

中文名稱 CAY10505
英文名稱 CAY10505
CAS 1218777-13-9
分子式 C14H8FNO3S
分子量 289.28
MOL 文件 1218777-13-9.mol
更新日期 2024/12/15 19:35:21
1218777-13-9 結(jié)構(gòu)式 1218777-13-9 結(jié)構(gòu)式

基本信息

中文別名
PI3KΓ抑制劑(CAY10505)
(5E)-5-[[5-(4-氟苯基)-2-呋喃基]亞甲基]-2,4-噻唑烷二酮
英文別名
CAY10505
CAY10505, >=98%
CAY10505 USP/EP/BP
(E)-5-((5-(4-fluorophenyl)furan-2-yl)methylene)thiazolidine-2,4-dione
(5E)-5-[[5-(4-Fluorophenyl)-2-furanyl]methylene]-2,4-thiazolidinedione
2,4-Thiazolidinedione, 5-[[5-(4-fluorophenyl)-2-furanyl]methylene]-, (5E)-
CAY10505 ( 5E)-5-[[5-(4-Fluorophenyl)-2-furanyl]methylene]-2,4-thiazolidinedione
所屬類別
生物化工:PI3K 抑制劑

物理化學(xué)性質(zhì)

密度1.466
儲(chǔ)存條件-20°C儲(chǔ)存
溶解度insoluble in EtOH; insoluble in H2O; ≥14.45 mg/mL in DMSO
酸度系數(shù)(pKa)7.21±0.20(Predicted)
形態(tài)固體
顏色Light yellow to yellow

常見問題列表

生物活性
CAY10505 是一種有效的選擇性 PI3Kγ 抑制劑,作用于神經(jīng)元細(xì)胞,IC50 為 30 nM。
靶點(diǎn)

PI3Kγ

30 nM (IC 50 , Neurons)

體外研究

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).

體內(nèi)研究

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.

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