您好,欢迎来到试剂仪器网! [登录] [免费注册]
试剂仪器网
位置:首页 > 产品库 > Vevorisertib
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:
 
Vevorisertib
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。
Vevorisertib图片
CAS NO:1416775-46-6
包装与价格:
包装价格(元)
100mg电议
250mg电议
500mg电议

产品名称
ARQ 751
产品介绍
Vevorisertib (ARQ 751) 是一种具有口服活性、有效和选择性的pan-AKT丝氨酸/苏氨酸激酶抑制剂,对AKT1(IC50=0.55 nM)、AKT2(IC50=0.81 nM) 和AKT3(IC50=1.31 nM) 有抑制作用。Vevorisertib 单体化合物或与其他抗癌化合物联用,可用于 PIK3CA/AKT/PTEN 突变的实体瘤研究。
生物活性

Vevorisertib (ARQ 751) is an orally active, potent and selectivepan-AKTserine/threonine kinaseinhibitor againstAKT1(IC50=0.55 nM),AKT2(IC50=0.81 nM), andAKT3(IC50=1.31 nM). Vevorisertib, as a single agent or in combination with other anti-cancer agents, can be used for the research of solid tumors with PIK3CA /AKT/PTENmutations[1][2][3][4].

IC50& Target[4]

Akt1

0.55 nM (IC50)

Akt2

0.81 nM (IC50)

Akt3

1.31 nM (IC50)

体外研究
(In Vitro)

Vevorisertib binds to wild-type AKT1 and mutant AKT1-E17K with Kdof 1.2 nM and 8.6 nM, respectively, and suppresses pAKT(S473) in 293T cells transiently transfected with AKT1-E17K[4].

体内研究
(In Vivo)

Vevorisertib (10~120 mg/kg) exerts dose-dependent anti-tumor activity in an AKT1-E17K mutant endometrial patient-derived xenograft (PDX) model. Vevorisertib shows a plasma half-life of 4 to 5 hours and no tissue accumulation[4].

Clinical Trial
分子量

586.73

Formula

C35H38N8O

CAS 号

1416775-46-6

运输条件

Room temperature in continental US; may vary elsewhere.

储存方式

Please store the product under the recommended conditions in the Certificate of Analysis.