A β-catenin-CBP protein-protein interaction inhibitor
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E-7386

Item No. 46299

Product Insert (PDF)Safety Data Sheet (SDS) (PDF)
Technical Information
Formal Name
(6S,9aS)-8-[[6-[3-(4-ethyl-1-piperazinyl)-1-azetidinyl]-2-pyridinyl]methyl]-6-[(2-fluoro-4-hydroxyphenyl)methyl]hexahydro-4,7-dioxo-N-(phenylmethyl)-2-(2-propen-1-yl)-2H-pyrazino[2,1-c][1,2,4]triazine-1(6H)-carboxamide
CAS Number
1799824-08-0
Molecular Formula
C39H48FN9O4
Formula Weight
725.9
Purity
≥98%
Formulation (Request formulation change)
A solid
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
Shipping & Storage Information
Storage
-20°C
Shipping
Room temperature in continental US; may vary elsewhere
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    5 mg

    $269

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    10 mg

    $457

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    25 mg

    $807

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    50 mg

    $1,345

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    Cayman Chemical
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    Product Description

    E-7386 is an inhibitor of the protein-protein interaction between β-catenin and CREB-binding protein (CBP).1 It inhibits reporter gene expression induced by β-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.

    WARNING This product is not for human or veterinary use.

    References & Product Citations
    Product Description References

    1. Yamada, K., Hori, Y., Inoue, S., 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. 81(4), 1052-1062 (2021).