E-7386

Research use only, not for human use.

E-7386 (E7386) is a potent, orally active modulator of CBP/beta-catenin.

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; 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, 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.

——

E-7386 is an orally active CBP/beta-catenin modulator which can induce T cells infiltration into tumor and enhance antitumor activity of anti-PD-1 mAb in Wnt1 tumor syngeneic mice model. E-7386 shows significant antitumor activity in Wnt1 model.Infiltration of T cells is limited in vehicle control group, but T cell infiltration into tumors is clearly observed in E-7386 treatment group.

E7386

Wnt/Notch/Hedgehog

Beta-catenin

Beta-catenin

——

——

1799824-08-0

725.87

C39H48FN9O4

>98% (HPLC)

In Vitro:?DMSO : 125 mg/mL (172.21 mM)

CCN1CCN(CC1)C2CN(C2)C3=CC=CC(=N3)CN4CC5N(C(C4=O)CC6=C(C=C(C=C6)O)F)C(=O)CN(N5C(=O)NCC7=CC=CC=C7)CC=C

(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

(-20℃)

With Ice Pack

≥ 2 years