E-7386

E-7386 is an inhibitor of the protein-protein interaction between beta-catenin and CREB-binding protein (CBP). It inhibits reporter gene expression induced by beta-catenin in ECC10 gastric small cell carcinoma cells that express mutant adenomatous polyposis coli and in HEK293 cells (APC, IC50s = 14.7 and 48.4 nM, respectively). E-7386 inhibits the growth of ECC10 cells (IC50 = 4.9 nM) and inhibits tumor growth in an ECC10 mouse xenograft model when administered at a dose of 25-50 mg/kg. It decreases the number of small intestine polyps in an Apc+/Min spontaneous colorectal adenoma mouse model and increases intratumoral CD8+ T cells and reduces tumor growth in a MMTV-Wnt1 isogenic mouse mammary tumor model.. SMILES: [H][C@]12CN(C([C@@H](N1C(CN(N2C(NCC3=CC=CC=C3)=O)CC=C)=O)CC4=C(F)C=C(O)C=C4)=O)CC5=CC=CC(N6CC(C6)N7CCN(CC7)CC)=N5. InChi Code: 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. InChi Key: ZGNKNLOBYFTGRG-GIWKVKTRSA-N