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E-7386

Chemical Structure : E-7386

CAS No.: 1799824-08-0

E-7386 (E7386)

Catalog No.: 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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Biological Activity

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.

Physicochemical Properties

M.Wt 725.87
Formula C39H48FN9O4
Appearance Solid
CAS No.
Storage
Solide Powder
-20 °C 12 Months; 4°C 6 Months
In Solvent
-80 °C 6 Months; -20°C 6 Months
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

References

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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