KRA-533 T38411
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 |
---|---|---|---|
2 mg | 10161-87-2 | ¥1,370.00 | 询底价 |
5 mg | 10161-87-2 | ¥2,320.00 | 询底价 |
1 mL | 10161-87-2 | ¥2,560.00 | 询底价 |
Product Introduction
Bioactivity
英文名: KRA-533
描述: KRA-533, a potent KRAS agonist, directly targets the GTP/GDP binding pocket within the KRAS protein, inhibiting GTP cleavage. This inhibition leads to the buildup of constitutively active GTP-bound KRAS, which subsequently activates both apoptotic and autophagic cell death pathways specifically in cancer cells.
体外活性: KRA-533 (10 μM; 48 hours; HCC827 cells) enhances KRAS activity to a greater extent[1]. KRA-533 (0~15 μM; 48 hours; H157 cells) enhances KRAS activity in a dose-dependent manner, which is associated increased levels of pERK, ratio of active caspase 3/procaspase 3 and PARP cleavage, leading to apoptotic cell death[1]. KRA-533 (10 μM; 10 days; H292 cells) mediates cell growth suppression than those without KRAS mutation. KRA-533 (5~15 μM) can directly bind to WT, G12C, G12D and G13D mutant KRAS proteins. KRA-533 activates WT KRAS to increase its activity in a dose-dependent manner. KRA-533 further enhances the activities of active KRAS mutants[1]. Western Blot Analysis[1]Cell Line: HCC827 cells Concentration: 10 μM Incubation Time: 48 hours Result: Enhanced KRAS activity to a greater extent. Apoptosis Analysis[1]Cell Line: H157 cells Concentration: 0~15 μM Incubation Time: 48 hours Result: Enhanced KRAS activity in a dose-dependent manner, which was associated increased levels of pERK, ratio of active caspase 3/procaspase 3 and PARP cleavage, leading to apoptotic cell death.
体内活性: KRA-533 (0~30 mg/kg; 28 days) suppresses tumor growth in a dose-dependent manner in lung cancer mutant KRAS xenografts and induces apoptosis and autophagy in tumor tissues in a dose-dependent manner[1]. KRA-533 shows optimal therapeutic index between 7.5 mg/kg and 30 mg/kg doses[1]. Animal Model: Nu/Nu nude mice[1]Dosage: 0~30 mg/kg Administration: I.p. Result: Suppressed tumor growth in a dose-dependent manner in lung cancer mutant KRAS xenografts and induced apoptosis and autophagy in tumor tissues in a dose-dependent manner.
存储条件: Powder: -20°C for 3 years | In solvent: -80°C for 1 year
关键字: KRA533 | KRA-533 | KRA 533
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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