产品信息
抗原名称
Wnt/β-catenin
商品描述
ICG-001 is a small-molecule antagonist of b-catenin/TCF-mediated transcription (IC50 = 3 uM) and specifically downregulates the expression of a subset of b-catenin/TCF-responsive genes. ICG-001 binds specifically to cyclic AMP response element-binding pro
分子量
548.63
纯度
>98%
可溶性
DMSO :100 mg/mL (182.27 mM)
Ethanol :10 mg/mL (18.22 mM)
Ethanol :10 mg/mL (18.22 mM)
外观
Off-white powder
In vitro(体外研究)
PRI-724 binds specifically to CBP but not the related transcriptional coactivator p300, thereby disrupting the interaction of CBP with β-catenin. Treatment with PRI-724 selectively induces apoptosis in colon carcinoma cells but not in normal colonic epithelial cells and reduces in vitro growth of colon carcinoma cells.
In vivo(体内研究)
PRI-724 exhibits antitumor activity in the mouse xenograft models of colon cancer. The initial results of the Phase I clinic trial of PRI-724 has been disclosed publically. The drug exhibits an acceptable toxicity profile with only one dose-limiting toxicity of grade 3 reversible hyperbilirubinaemia. An Open-Label dose-escalation phase I/II study of PRI-724 for patients with advanced myeloid malignancies is still ongoing.
背景
别名
ICG001;ICG 001
分子式
C33H32N4O4
CAS号
780757-88-2;847591-62-2
制备和贮存
保存方式
Store at -20℃ for one year(Powder);Store at 2-4℃ for two weeks;Store at -20℃ for six months after dissolution.
参考图片
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