E-7386 (E7386)

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: C₃₉H₄₈FN₉O_4.
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.