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Background Information:
E-7386 (E7386) is a first-in-class orally active specific modulator of CBP/beta-catenin. 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 (ref 1).
Reference:
1. Yusaku Hori, et al. E7386, an orally active CBP/beta-catenin modulator, induces T cells infiltration into tumor and enhances antitumor activity of anti-PD-1 mAb in Wnt1 tumor syngeneic mice model. Cancer Res 2017;77(13 Suppl):Abstract nr 5172.
APIM050299: E-7386 (E7386)
CAS No.: 1799824-08-0.
Molecular Formula: C39H48FN9O4.
Molecular Weight: 725.9.
Purity: >99% by Achiral and Chiral HPLCs.
QC: Achiral and Chiral HPLCs, MS, NMR, and Quantitative Elemental Analysis Report.
Solubility: Refer to certificate of analysis.
Storage: Refer to certificate of analysis.
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