KRA-533

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上海金畔生物科技有限公司为生命科学和医药研发人员提供生物活性分子抑制剂、激动剂、特异性抑制剂、化合物库、重组蛋白，专注于信号通路和疾病研究领域。

KRA-533 

KRA-533 是一种有效的 KRAS 激动剂。KRA-533 与 KRAS 蛋白中的 GTP/GDP binding pocket 结合，防止 GTP 切割，导致 GTP 结合 KRAS 的组成性活性积累，触发癌细胞中凋亡和自噬细胞死亡途径。

KRA-533

KRA-533 Chemical Structure

CAS No. : 10161-87-2

规格 价格 是否有货
5 mg ￥2800 询问价格 & 货期
10 mg ￥4200 询问价格 & 货期
25 mg ￥8000 询问价格 & 货期
50 mg ￥11900 询问价格 & 货期

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生物活性

KRA-533 is a potent KRAS agonist. KRA-533 binds to the GTP/GDP binding pocket in the KRAS protein to prevent GTP cleavage, resulting in the accumulation of constitutively active GTP-bound KRAS that triggers both apoptotic and autophagic cell death pathways in cancer cells.

IC50 & Target

KRAS[1]
体外研究
(In Vitro)

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].

上海金畔生物科技有限公司 has not independently confirmed the accuracy of these methods. They are for reference only.

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.

体内研究
(In Vivo)

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].

上海金畔生物科技有限公司 has not independently confirmed the accuracy of these methods. They are for reference only.

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.

分子量

314.18

Formula

C13H16BrNO3
CAS 号

10161-87-2
运输条件

Room temperature in continental US; may vary elsewhere.
储存方式
Powder -20°C 3 years
In solvent -80°C 6 months
-20°C 1 month
参考文献

  • [1]. Xu K, et al. Small Molecule KRAS Agonist for Mutant KRAS Cancer Therapy [published correction appears in Mol Cancer. 2020 May 20;19(1):93]. Mol Cancer. 2019;18(1):85. Published 2019 Apr 10.

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