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E-7386
- Optical Purity: 99% e.e.
- Soluble in 0.1N HCl(aq) and DMSO
- MF: C39H48FN9O4
- MW: 725.85
Description
E-7386 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.
More Information
| Parent CAS No. | 1799824-08-0 |
|---|---|
| Chemical Name | (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-dioxooctahydro-1H-pyrazino[2,1-c][1,2,4]triazine-1-carboxamide |
| extra_info | Sold in collaboration with Chemietek |
| SMILES | N1(CC2C=CC=C(N3CC(N4CCN(CC)CC4)C3)N=2)C[C@]2([H])N(C(=O)NCC3C=CC=CC=3)N(CC=C)CC(=O)N2[C@@H](CC2C(F)=CC(O)=CC=2)C1=O |&1:21,42,r| |
| MFCD | N.A. |
| InChi | InChI=1S/C39H48FN9O4/c1-3-15-47-27-37(51)48-34(20-29-13-14-32(50)21-33(29)40)38(52)46(26-36(48)49(47)39(53)41-22-28-9-6-5-7-10-28)23-30-11-8-12-35(42-30)45-24-31(25-45)44-18-16-43(4-2)17-19-44/h3,5-14,21,31,34,36,50H,1,4,15-20,22-27H2,2H3,(H,41,53)/t34-,36-/m0/s1 |
| InChiKey | ZGNKNLOBYFTGRG-GIWKVKTRSA-N |
| CID | 91810345 |
| Short Description | CBP/beta-catenin modulator |
References
- 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, Abstract nr 5172.
- K. Yamada et al E7386, a Selective Inhibitor of the Interaction between β-Catenin and CBP, Exerts Antitumor Activity in Tumor Models with Activated Canonical Wnt Signaling. Cancer Res. 2021, 81, 1052-1062.
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