KRA-533|cas:10161-87-2|西域试剂

KRA-533,98.94%

产品编号：Bellancom-138188| CAS NO：10161-87-2| 分子式：C₁₃H₁₆BrNO₃| 分子量：314.18

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货号	价格	库存与货期
Bellancom-138188	￥2800.00	杭州北京（现货）
Bellancom-138188	￥4200.00	杭州北京（现货）
Bellancom-138188	￥8000.00	杭州北京（现货）
Bellancom-138188	￥11900.00	杭州北京（现货）

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KRA-533

产品介绍

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。

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.

体外研究

KRA-533 (10 μM; 48 hours; HCC827 cells) enhances KRAS activity to a greater extent.
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.
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.

西域 has not independently confirmed the accuracy of these methods. They are for reference only.

Western Blot Analysis

Cell Line:	HCC827 cells
Concentration:	10 μM
Incubation Time:	48 hours
Result:	Enhanced KRAS activity to a greater extent.

Apoptosis Analysis

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; i.p.; 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.
KRA-533 shows optimal therapeutic index between 7.5 mg/kg and 30 mg/kg doses.

西域 has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model:	Nu/Nu nude mice (mutant KRAS xenografts)
Dosage:	0~30 mg/kg
Administration:	i.p.; 28 days
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.

体内研究

西域 has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model:	Nu/Nu nude mice (mutant KRAS xenografts)
Dosage:	0~30 mg/kg
Administration:	i.p.; 28 days
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.

体内研究

西域 has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model:	Nu/Nu nude mice (mutant KRAS xenografts)
Dosage:	0~30 mg/kg
Administration:	i.p.; 28 days
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.

性状

Solid

溶解性数据

In Vitro:

DMSO : 250 mg/mL (795.72 mM; Need ultrasonic)

配制储备液

浓度溶剂体积质量	1 mg	5 mg	10 mg

1 mM	3.1829 mL	15.9144 mL	31.8289 mL
5 mM	0.6366 mL	3.1829 mL	6.3658 mL
10 mM	0.3183 mL	1.5914 mL	3.1829 mL

请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液；一旦配成溶液，请分装保存，避免反复冻融造成的产品失效。
储备液的保存方式和期限：-80°C, 6 months; -20°C, 1 month。-80°C 储存时，请在 6 个月内使用，-20°C 储存时，请在 1 个月内使用。

运输条件

Room temperature in continental US; may vary elsewhere.

储存方式