E-7386 is a selective inhibitor that inhibits the interaction between CBP/β-catenin with an IC50 value of 0.0484 μM in HEK293 cells.

 

Brand: BCM

 

Target: Epigenetic Reader Domain

 

Signaling Pathways: Chromatin/Epigenetic

 

In Vivo: E-7386 is an oral active CBP/ -catenin regulator, which can induce T cells to infiltrate into the tumor in the Wnt1 tumor cogene mouse model and enhance the anti-tumor activity of anti-PD-1 monoclonal antibody.In the Wnt1 model, t-cell infiltration in the vehicle control group was limited, while t-cell infiltration in the E-7386 treatment group was obvious, and E-7386 showed significant anti-tumor activity.

 

pKa: 8.92±0.20(Predicted)

 

Solubility: Soluble in DMSO; soluble in Ethanol. Insoluble in Water.

 

Isomeric SMILES: CCN1CCN(CC1)C2CN(C2)C3=CC=CC(=N3)CN4C[C@H]5N([C@H](C4=O)CC6=C(C=C(C=C6)O)F)C(=O)CN(N5C(=O)NCC7=CC=CC=C7)CC=C  

 

InChIKey: ZGNKNLOBYFTGRG-GIWKVKTRSA-N  

 

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

 

Attribute
[Chem Name]	(6S,9aS)-N-benzyl-8-[[6-[3-(4-ethylpiperazin-1-yl)azetidin-1-yl]pyridin-2-yl]methyl]-6-[(2-fluoro-4-hydroxyphenyl)methyl]-4,7-dioxo-2-prop-2-enyl-3,6,9,9a-tetrahydropyrazino[2,1-c][1,2,4]triazine-1-carboxamide
[Synonym]	E-7386
[CAS No.]	1799824-08-0
[MDL No.]	MFCD31619284
[Formula]	C39H48FN9O4
[Molecular]	725.85
[Form]	Solid Powder
[Storage]	Keep in dark place. Sealed in dry, 2-8°C

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