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 > NVP-TNKS656
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:
 
NVP-TNKS656
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。
NVP-TNKS656图片
CAS NO:1419949-20-4
包装与价格:
包装价格(元)
2 mg电议
5 mg电议
10 mg电议
25 mg电议
50 mg电议
100 mg电议
1 mL*10 mM(in DMSO)电议

产品名称
TNKS656
产品介绍
NVP-TNKS656 是一种可口服的选择性TNKS2抑制剂,IC50值为 6 nM。

产品描述

NVP-TNKS656 is a highly potent, selective, and orally active TNKS2 inhibitor.

体外活性

In vitro, NVP-TNKS656 shows low to moderate microsomal ER values across species and high solubility. [1] In PI3K or AKT inhibitor-resistant cells, NVP-TNKS656 blocks Wnt/β-Catenin pathway and promotes apoptosis. [2]

体内活性

In mice, NVP-TNKS656 displays low clearance and volume of distribution, and exhibits good exposure and moderate oral bioavailability. In MMTV-Wnt1 tumor bearing athymic nude mice, NVP-TNKS656 (350 mg/kg, p.o.) stabilizes Axin1 protein and reduces the Wnt/beta-catenin target gene Axin2 mRNA level by 70-80%. [1] In colorectal cancer PDX models, NVP-TNKS656 reduces nuclear β-catenin, reverts such resistance, and represses tumor growth. [2]

Cas No.

1419949-20-4

分子式

C27H34N4O5

分子量

494.592

别名

TNKS656

储存和溶解度

H2O:<1 mgml
Ethanol:10 mg/mL(20.21 mM),warming
DMSO:93 mg/mL (188 mM)
Powder: -20°C for 3 years
In solvent: -80°C for 2 years