计算溶液所需的质量、体积或浓度。
为什么选择此级别
，适用于对基线干扰要求严格的色谱和分析工作流程。
储存与运输
-80℃储存。特低温运输 。请查阅批次 COA 获取详细规格。
质量文档
SDS、COA、产品数据表及规格说明书均可下载。可通过批号查询获取批次 COA。
文献证明
在色谱分析、有机合成和交叉偶联反应领域已被 0 篇同行评审文献引用。
概述
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.
In Vitro
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. MCE has not independently confirmed the accuracy of these methods. They are for reference only. Western Blot AnalysisCell Line: HCC827 cells Concentration: 10 μM Incubation Time: 48 hours Result: Enhanced KRAS activity to a greater extent. Apoptosis AnalysisCell 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.
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 . MCE 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.
IC50& Target:KRAS
规格
规格或纯度
10mM in DMSO
英文名称
KRA-533
生化机理
KRA-533 是一种强效的 KRAS 激动剂。KRA-533 与 KRAS 蛋白中的 GTP/GDP 结合袋结合，阻止 GTP 的裂解，从而导致组成型活性 GTP 结合型 KRAS 的积累，引发细胞凋亡和自噬。
储存条件
-80℃储存
运输条件
特低温运输
作用类型
激动剂
名称和识别符
分子类型
小分子
Isomeric SMILES
C1=CC(=CC=C1CCCCNC(=O)CBr)C(=O)O
关联CAS
PubChem CID
NSC Number
112533
分子量
314.18
技术文档
高级数据
质检证书（CoA,COO,BSE/TSE 和分析图谱)
C of A & Other Certificates(BSE/TSE, COO):
输入批号以搜索分析图谱:
溶液计算器
常见问题
本产品应如何储存？
请于?80 °C条件下保存。需超低温保存以维持规定的有效期。
本产品如何运输？
本产品采用干冰配冷袋冷冻运输。收货后请立即拆包，并按上述储存条件保存；处理干冰时请戴隔热手套并保持通风。
本产品的 CAS 号、分子式和分子量是多少？
本产品的 CAS 号为 10161-87-2，分子式为 C13H16BrNO3，分子量为 314.18 g/mol。
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