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

E-7386
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WARNING: This product is for research use only, not for human or veterinary use.

MedKoo CAT#: 462568

CAS#: 1799824-08-0

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

Chemical Structure

E-7386

CAS# 1799824-08-0

Product data Instruction

Theoretical Analysis

MedKoo Cat#: 462568
Name: E-7386
CAS#: 1799824-08-0
Chemical Formula: C39H48FN9O4
Exact Mass: 725.38
Molecular Weight: 725.870
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	2 Weeks
10mg	USD 550	2 Weeks
25mg	USD 1250	2 Weeks
50mg	USD 2050	2 Weeks
Bulk inquiry Welcome, Customer: Please do not inquire quote if your intended use is for a patient since our products are for research use and for chemical synthesis use, not for human use . For in-stock products, we listed price in the web page. You may inquire prices for which sizes were not listed. If no price is listed, this means the product is not in stock at the moment, which may be available via custom synthesis. For cost-effective reason, minimum order of 1g is requested (typically very expensive). The lead time is usually 2-4 months. Quote of less than 1g will not be provided. MedKoo may not offer quote for below reasons: (1) current available synthetic method appears to be extremely expensive which is obviously not affordable to most customers; (2) Key raw material to make the product is temporally not available; (3) DEA controlled substances; (4) the product is under patent protection in customer’s country.

Synonym: E-7386; E7386; E 7386

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:

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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

Solubility Data

	Solvent	Max Conc. mg/mL	Max Conc. mM
Solubility
	DMSO	125.0	172.21

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:	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 vivo 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.

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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.

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