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 > DT-061
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:
 
DT-061
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。
DT-061图片
CAS NO:1809427-19-7
包装与价格:
包装价格(元)
10mM (in 1mL DMSO)电议
5mg电议
10mg电议

产品介绍
DT-061是一种具有口服生物活性的、蛋白磷酸酶2A(PP2A)的激活剂,可用于治疗KRAS突变和MYC驱动的肿瘤。
Cas No.1809427-19-7
Canonical SMILESO=S(C1=CC=C(OC(F)(F)F)C=C1)(N[C@H]2[C@H](O)[C@@H](N3C4=C(C=CC=C4)OC5=CC=CC=C35)CCC2)=O
分子式C25H23F3N2O5S
分子量520.52
溶解度DMSO : 125 mg/mL (240.14 mM);Water :< 0.1 mg/mL (insoluble)
储存条件Store at -20°C
General tipsFor obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while.
Shipping ConditionEvaluation sample solution : ship with blue ice
All other available size: ship with RT , or blue ice upon request
产品描述

DT-061 is an orally bioavailable activator of protein phosphatase 2A (PP2A) and could be applied in the therapy of KRAS-mutant and MYC-driven tumorigenesis[1]. PP2A[1].

DT-061 (5 mg/kg, oral gavage, 4 weeks) shows single-agent activity in inhibiting H358 or H441 xenograft growth. Additionally, the combination of DT-061 and AZD6244 is more significantly efficient[1]. Animal Model: 6- to 8-week-old male BALB/c nu/nu mice injected with H441 cells (5 × 106)[1].

[1]. Kauko O, et al. PP2A inhibition is a druggable MEK inhibitor resistance mechanism in KRAS-mutant lung cancer cells. Sci Transl Med. 2018 Jul 18;10(450). pii: eaaq1093.