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JW74
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。
JW74图片
CAS NO:863405-60-1
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
200 mg电议
500 mg电议
1 mL*10 mM(in DMSO)电议

产品介绍
JW74 能够拮抗 LiCl 诱导的经典 Wnt 信号激活 (IC50: 420 nM)。

产品描述

JW74 antagonizes LiCl-induced activation of the canonical Wnt signaling (IC50: 420 nM).

体外活性

Ki-67 expression is reduced from 97.5% in DMSO-treated cells to 86.7% in JW74-treated cells. Relative to DMSO-treated cells, the cellular viability of U2OS cells treated for 72 h treatment with 10 μM JW74 is reduced to 80%. The effect of tankyrase inhibition on cellular viability is tested by performing an MTS assay. Flow cytometry is also performed to determine the expression marker Ki-67 in U2OS following 48 h treatment with DMSO or 10 uM JW74 [2]. JW74 displays a reduction of canonical Wnt signaling in the ST-Luc assay (IC50: 790 nM) [1].

体内活性

The in vivo efficacy of JW74 is tested using SW480 cell xenografts. A relatively high dose of JW74 (150 or 300 mg/kg) is used because of a rapid compound degradation in the organism as indicated in the human liver microsome analysis (t1/2=2.5 minutes) and in pharmacokinetic analyses (after peroral injections: t1/2=30 minutes and intravenous injections: t1/2=15 minutes). JW74 concentration in tumors is in the range 4.2 to 72.1 μmol/kg for JW74 150 mg/kg, 1.9 to 11.1 μmol/kg for JW74 300 mg/kg, and 2.8 μM in plasma for both doses [1].

Cas No.

863405-60-1

分子式

C24H20N6O2S

分子量

456.52

储存和溶解度

DMSO:45 mg/mL (98.57 mM)
Powder: -20°C for 3 years
In solvent: -80°C for 2 years