E-7386 | CAS#1799824-08-0 | CBP/beta-catenin modulator

MedKoo Cat#: 462568 | Name: E-7386

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Description:

WARNING: This product is for research use only, not for human or veterinary use.

E-7386 is an orally active CBP/beta-catenin modulator.

Chemical Structure

E-7386

CAS#1799824-08-0

Theoretical Analysis

MedKoo Cat#: 462568

Name: E-7386

CAS#: 1799824-08-0

Chemical Formula: C39H48FN9O4

Exact Mass: 725.3813

Molecular Weight: 725.87

Elemental Analysis: C, 64.53; H, 6.67; F, 2.62; N, 17.37; O, 8.82

Price and Availability

Size	Price	Availability
5mg	USD 350.00	2 Weeks
10mg	USD 600.00	2 Weeks
25mg	USD 1,250.00	2 Weeks
50mg	USD 2,050.00	2 Weeks

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Related CAS #

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Synonym

E-7386; E7386; E 7386; NSC820052; NSC 820052; NSC-820052

IUPAC/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-dioxohexahydro-2H-pyrazino[2,1-c][1,2,4]triazine-1(6H)-carboxamide

InChi Key

ZGNKNLOBYFTGRG-GIWKVKTRSA-N

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

SMILES Code

O=C(N([C@](CN1CC2=NC(N3CC(N4CCN(CC)CC4)C3)=CC=C2)([H])N5[C@@H](CC6=CC=C(O)C=C6F)C1=O)N(CC=C)CC5=O)NCC7=CC=CC=C7

Appearance

Solid powder

Purity

>98% (or refer to the Certificate of Analysis)

Shipping Condition

Shipped under ambient temperature as non-hazardous chemical. This product is stable enough for a few weeks during ordinary shipping and time spent in Customs.

Storage Condition

Dry, dark and at 0 - 4 C for short term (days to weeks) or -20 C for long term (months to years).

Solubility

Soluble in DMSO

Shelf Life

>3 years if stored properly

Drug Formulation

This drug may be formulated in DMSO

Stock Solution Storage

0 - 4 C for short term (days to weeks), or -20 C for long term (months).

HS Tariff Code

2934.99.9001

More Info

Product Data

Product Data

Instruction

View handling instruction

Biological target:

E-7386 is an orally active CBP/beta-catenin modulator.

In vitro activity:

E7386 treatment for 6 hours inhibited TCF/LEF luciferase activity in a dose-dependent manner in both cell lines. The IC50 value of E7386 in HEK293 and ECC10 cells was 0.0484 and 0.0147 μmol/L, respectively. Reference: Cancer Res. 2021 Feb 15;81(4):1052-1062. https://cancerres.aacrjournals.org/content/81/4/1052.long

In vivo activity:

E7386 showed in vivo antitumor activity in a dose-dependent manner, and significantly inhibited tumor growth when administered at 25 or 50 mg/kg (Fig. 3A) without any significant changes in body weight (Fig. 3B). E7386 treatment for 14 days at 12.5, 25, or 50 mg/kg also showed significant dose-dependent antitumor activity in vivo without any significant changes in body weight (Supplementary Fig. S6A). In contrast, 100 mg/kg of ICG-001 showed only slight antitumor activity and this observation was not statistically significant (Supplementary Fig. S6B). Reference: Cancer Res. 2021 Feb 15;81(4):1052-1062. https://cancerres.aacrjournals.org/content/81/4/1052.long

	Solvent	mg/mL	mM
Solubility
	DMSO	125.0	172.21

Note: There can be variations in solubility for the same chemical from different vendors or different batches from the same vendor. The following factors can affect the solubility of the same chemical: solvent used for crystallization, residual solvent content, polymorphism, salt versus free form, degree of hydration, solvent temperature. Please use the solubility data as a reference only. Warming and sonication will facilitate dissolving. Still have questions? Please contact our Technical Support scientists.

Preparing Stock Solutions

The following data is based on the product molecular weight 725.87 Batch specific molecular weights may vary from batch to batch due to the degree of hydration, which will affect the solvent volumes required to prepare stock solutions.

Concentration / Solvent Volume / Mass	1 mg	5 mg	10 mg
1 mM	1.15 mL	5.76 mL	11.51 mL
5 mM	0.23 mL	1.15 mL	2.3 mL
10 mM	0.12 mL	0.58 mL	1.15 mL
50 mM	0.02 mL	0.12 mL	0.23 mL

Formulation protocol:

1. Yamada K, Hori Y, Inoue S, Yamamoto Y, Iso K, Kamiyama H, Yamaguchi A, Kimura T, Uesugi M, Ito J, Matsuki M, Nakamoto K, Harada H, Yoneda N, Takemura A, Kushida I, Wakayama N, Kubara K, Kato Y, Semba T, Yokoi A, Matsukura M, Odagami T, Iwata M, Tsuruoka A, Uenaka T, Matsui J, Matsushima T, Nomoto K, Kouji H, Owa T, Funahashi Y, Ozawa Y. 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 Feb 15;81(4):1052-1062. doi: 10.1158/0008-5472.CAN-20-0782. Epub 2021 Jan 6. PMID: 33408116.

In vitro protocol:

In vivo protocol:

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.