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首页-小分子抑制剂&激动剂-Wnt/Notch/Hedgehog-Beta-catenin-E-7386
E-7386

Chemical Structure : E-7386

CAS No.: 1799824-08-0

E-7386 (E7386)

货号: PC-35329Not For Human Use, Lab Use Only.

E-7386 (E7386) is a potent, orally active modulator of CBP/beta-catenin, disrupts the interaction and inhibits canonical Wnt signaling pathway /TCF reporter gene activity in LiCl-stimulated HEK-293 and MDA-MB-231 with IC50 of 55 and 73 nM, respectively.

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10 mg ¥2380 In stock
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纯度 & COA & 质检文件 纯度: >98% (HPLC) Select Batch:

生物&药学活性

E-7386 (E7386) is a potent, orally active modulator of CBP/beta-catenin, disrupts the interaction and inhibits canonical Wnt signaling pathway /TCF reporter gene activity in LiCl-stimulated HEK-293 and MDA-MB-231 with IC50 of 55 and 73 nM, respectively.
E7386 exhibits anti-tumor activity in vitro tumor proliferation panel against 28 human tumor cell lines.
E7386 modulates the expression of Wnt signaling pathway related genes including AXIN2 and other genes, significantly suppressed the number of polyposis in a dose dependent manner at the dose 8.5-50 mg/kg, also significantly changed the expressions of Wnt related genes in whisker follicle of ApcMin/+mice model.

物理化学性质&存储条件

分子量 725.87
分子式 C39H48FN9O4
外观性状 Solid
CAS No.
储存条件
固体粉末
-20 °C 12 个月; 4°C 6 个月
配置液
-80 °C 6 个月; -20°C 6 个月
Shipping
Solubility

10 mM in DMSO

Chemical Name/SMILES

(6S,9aS)-2-allyl-N-benzyl-8-((6-(3-(4-ethylpiperazin-1-yl)azetidin-1-yl)pyridin-2-yl)methyl)-6-(2-fluoro-4-hydroxybenzyl)-4,7-dioxohexahydro-2H-pyrazino[2,1-c][1,2,4]triazine-1(6H)-carboxamide

参考文献

1. Kazuhiko Yamada, et al. Abstract 5177: E7386 : First-in-class orally active CBP/beta-catenin modulator as an anticancer agent. AACR 2017.

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