您好,欢迎来到化工原料网! [登录] [免费注册]
化工原料网
位置:首页 > 产品库 > KRA-533
立即咨询
咨询类型:
     
*姓名:
*电话:
*单位:
Email:
*留言内容:
请详细说明您的需求。
*验证码:
 
KRA-533
本产品不向个人销售,仅用作科学研究,不用于任何人体实验及非科研性质的动物实验。
KRA-533图片
规格:98%
分子量:314.18
包装与价格:
包装价格(元)
5mg电议
10mg电议
25mg电议
50mg电议

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。
货号:ajcx37848
CAS:10161-87-2
分子式:C13H16BrNO3
分子量:314.18
溶解度:N/A
纯度:98%
存储:Store at -20°C
库存:现货

Background:

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.

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].

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].

[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.