化合物Vevorisertib trihydrochloride T38846
品牌 | 厂商性质 | 产地 | 货期 |
---|---|---|---|
TargetMol | 生产商 | 美国 | 现货 |
性能特点
生化试剂,可用于动物细胞实验
规格 | CAS号 | 价格 | 操作 |
---|---|---|---|
10 mg | 1416775-08-0 | ¥1,690.00 | 询底价 |
100 mg | 1416775-08-0 | ¥5,470.00 | 询底价 |
50 mg | 1416775-08-0 | ¥3,970.00 | 询底价 |
5 mg | 1416775-08-0 | ¥1,130.00 | 询底价 |
1 mg | 1416775-08-0 | ¥469.00 | 询底价 |
25 mg | 1416775-08-0 | ¥2,880.00 | 询底价 |
Product Introduction
Bioactivity
英文名: Vevorisertib trihydrochloride
描述: Vevorisertib trihydrochloride(ARQ 751 trihydrochloride) 是一种具有选择性和有效性的 pan-AKT 和 AKT1-E17K 突变抑制剂,抑制 AKT1 、AKT2 和 AKT3 。 Vevorisertib trihydrochloride 可用于研究肝癌和晚期实体瘤。
体外活性: Vevorisertib trihydrochloride (0、12、33、111、333、1000 nM,2小时)抑制AKT1-E17K的磷酸化[2]。无论是否存在生长因子,Vevorisertib trihydrochloride (1 μM,2小时;NIH 3T3细胞转染pcDNAAKT-WT-GFP或pcDNA-E17K-GFP)均能抑制AKT-WT和AKT1-E17K的质膜转移[2]。Vevorisertib trihydrochloride (5 μM)表现出对全长AKT1 57%的抑制作用[1]。Vevorisertib trihydrochloride (0、0.012、0.037、0.11、0.33、1 μM;2小时)对mTORC1及AKT直接底物(包括PRAS40、GSK3β、FOXO、BAD及AS160)显示出剂量依赖性效应,适用于癌细胞系[2]。Vevorisertib trihydrochloride 对食管癌、乳腺癌和头颈癌细胞具有抗增殖作用(GI 50 < 1 μM)[1]。在PIK3CA突变细胞系中,Vevorisertib trihydrochloride 展现强烈的抗增殖活性[2]。Vevorisertib trihydrochloride (MK-4440)/伊马替尼美西酸盐(IM)组合能促进胃肠间质瘤(GIST)细胞周期阻滞,并增加细胞死亡率[1]。再次强调,在PIK3CA突变细胞系中,Vevorisertib trihydrochloride 显著抑制细胞增殖[2]:乳腺癌细胞系的GI 50 (nM)数据表明,与PIK3CA、ER、PR、HER2状态相关的各细胞系均对Vevorisertib trihydrochloride 敏感。Western Blot分析[1][2]显示,Vevorisertib trihydrochloride 能够抑制AKT1-E17K的磷酸化,并对mTORC1及AKT直接底物表现出剂量依赖性抑制效应,展现了其对各类癌细胞系具有广泛的抑制作用。
体内活性: Vevorisertib trihydrochloride (25, 50 and 75 mg/kg; p.o.; 5 days dosing followed by a 4 day dosing holiday for 20 days) shows potent tumor growth inhibition of 68, 78 and 98%, respectively [2] . Vevorisertib trihydrochloride (5, 10, 20, 40, 80, and 120 mg/kg; p.o. daily for ten days) shows tumor growth inhibition of 29, 33, 50, 73, 83, and 92%, respectively [2] . Vevorisertib trihydrochloride reachs C max plasma concentrations of ≥2 μM [2] . Vevorisertib trihydrochloride is generally well-tolerated at dose levels up to 120 mg/kg [2] . Vevorisertib trihydrochloride (MK-4440)/IM combination shows superior efficacy in an IM-sensitive preclinical model of GIST compared with either single agent [1] . Animal Model: Endometrial PDX mouse xenograft models (AKT1-E17K mutation tumor fragments subcutaneously implanted in athymic nude mice; tumor volume of approximately 200 mm 3 ) [2] Dosage: 25, 50 and 75 mg/kg Administration: p.o.; 5 days dosing followed by a 4 day dosing holiday for 20 days Result: Showed potent tumor growth inhibition of 68, 78 and 98%, respectively. Animal Model: AN3CA mouse xenograft models (female NCr nu/nu mice with 250 mm 3 tumors size) [2] Dosage: 5, 10, 20, 40, 80, and 120 mg/kg Administration: p.o.; daily for ten days Result: Showed tumor growth inhibition of 29, 33, 50, 73, 83, and 92%, respectively.
存储条件: store at low temperature,keep away from direct sunlightPowder: -20°C for 3 years | In solvent: -80°C for 1 year
溶解度: H2O : 20 mg/mL (28.73 mM)
DMSO : 100 mg/mL (143.66 mM)
关键字: ARQ-751 Trihydrochloride | ARQ751 Trihydrochloride | ARQ751 | ARQ-751 | ARQ 751 | Vevorisertib | Vevorisertib trihydrochloride
相关产品: PI3K-IN-48 | Dalbergioidin | Afuresertib hydrochloride | Norathyriol | 6'-GNTI dihydrochloride | Artemisinin | TD52 | AKT-IN-2 | MK-2206 free base | Kazinol B
相关库: Kinase Inhibitor Library | Inhibitor 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