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E-7386 (E7386) is a first-in-class orally active specific inhibitor of CBP/β-catenin complex, and a modulator of Wnt signaling pathway. It disrupts the interaction and inhibits canonical Wnt signaling pathway /TCF reporter gene activity in LiCl-stimulated HEK-293 and MDA-MB-231 in a dose-dependent manner, with IC50 of 55 and 73 nM, respectively; exhibits anti-tumor activity in vitro tumor proliferation panel against 28 human tumor cell lines; modulates the expression of Wnt signaling pathway related genes including AXIN2 and other genes. Oral administration of E7386 significantly suppressed the number of polyposis in a dose dependent manner at the dose range from 8.5 to 50 mg/kg. It also significantly changed the expressions of Wnt related genes in whisker follicle of ApcMin/+mice model (refs 1, 2).
Catalog NO: CT-E7386
Synonym: E-7386
CAS NO: 1799824-08-0
Mol. Formula: C39H48FN9O4
MW: 725.9
** in vivo Quality Material. >99% by Achiral and Chiral HPLCs (Attached). An enantiomerically pure single isomer (100% by Chiral HPLC). Anhydrous, validated by a spot-on Elemental Analysis. Bulk. Same Day Shipping.