化合物BLU2864 T60170

Product Introduction
Bioactivity


英文名: BLU2864

描述: BLU2864 是一种具有口服活性的、高选择性的、ATP 竞争性的 PRKACA 抑制剂 ，IC50值为0.3 nM。BLU2864 具有抗肿瘤活性，具有用于癌症和多囊肾的研究潜力。

体外活性: BLU2864 (40 nM and 200 nM; 5 d) shows inhibition of forskolin -induced cystogenesis in vitro[1]. Cell Viability Assay [1] Cell Line: mIMCD3 cells Concentration: 40 nM and 200 nM Incubation Time: 5 days Result: Inhibited forskolin induced in vitro cystogenesis of mIMCD3 cells cultured in Matrigel by 72% and 100% at 40 and 200 nM concentrations, respectively, relative to control.

体内活性: BLU2864 (oral gavage; 45 mg/kg; once daily; 5 d) shows inhibition of renal PKA activity in Pkd1 RC/RC mice [1]. BLU2864 (oral gavage; 30 mg/kg; once daily; 5 d) inhibits PKA activity and ameliorates PKD in Pkd1 RC/RC mice [1]. BLU2864 (oral gavage; 30 mg/kg and 75 mg/kg; once daily; 34 d) reduces FLC tumor growth in vivo [2]. Animal Model: Pkd1 RC/RC mice [1] Dosage: 45 mg/kg Administration: Oral gavage; 45 mg/kg; once daily; 5 days Result: Suppressed kidney basal and total PKA activities by 74% and 87% at 3 hours and by 46% and 56% at 15 hours, respectively, in the BLU2864-treated mice compared with controls. Animal Model: Pkd1 RC/RC mice [1] Dosage: 30 mg/kg Administration: Oral gavage; 30 mg/kg; once daily; 5 days Result: Showed higher urine outputs at 15 weeks in the BLU2864-treated mice than in the controls. Showed lower kidney weights, kidney volumes as percent of body weights, and cyst indices. Showed renal basal and total PKA activities by 69% and 84% lower in the BLU2864-treated mice compared with controls. Animal Model: Mice harboring FLC PDX tumors [2] Dosage: 30 mg/kg and 75 mg/kg Administration: Oral gavage; 30 mg/kg and 75 mg/kg; once daily; 34 days Result: Inhibited tumor growth by 48.5% (P=0.003) and by 45.3% (P=0.0005), respectively, at day 34.

存储条件: Powder: -20°C for 3 years | In solvent: -80°C for 1 year

溶解度: DMSO : 50 mg/mL (110.51 mM)


关键字: BLU-2864 | BLU2864 | BLU 2864

相关库: Anti-Cancer Compound Library | Bioactive Compounds Library Max | Inhibitor Library | Kinase Inhibitor Library | Anti-Cancer Active Compound Library | Bioactive Compound Library

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注：该产品未在中华人民共和国食品药品监督管理部门申请医疗器械注册和备案，不可用于临床诊断或治疗等相关用途