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產(chǎn)品名稱

CPI 0610

產(chǎn)品貨號(hào)

Axon 2594 CAS [1380087-89-7] MF C20H16ClN3O2MW 365.81 Purity: 99% Soluble in DMSO Description Selective and metabolically stable inhibitor of the BET family of bromodomains (BET-BRD; IC50 values 0.12 - 0.17 μM and 0.22 μM for inhibition of BD-1 of BRD2-4 and BRDT, respectively), demonstrating a correlation between BET-driven reduction in MYC gene expression and tumor growth inhibition in a xenograft study. CPI 0610 displays essentially no activity in TR-FRET- or AlphaLisabased assays against the bromodomains of CBP, BRD9, BRPF1, PCAF, BRG1, ATAD2, TRIM24, BRD8 (IC50 value > 15 μM), and no meaningful inhibition in a CEREP express panel of about 50 GPCRs, ion channels, and transporters. *Constellation Pharmaceuticals Inc compound; sold under agreement with Constellation Pharmaceuticals Inc.

產(chǎn)品價(jià)格

現(xiàn)貨詢價(jià)，電話：010-67529703

產(chǎn)品規(guī)格

產(chǎn)品品牌

axonmedchem

產(chǎn)品概述

產(chǎn)品詳情

CPI 0610

Based on 133 reference(s) in Google Scholar 8 10 133

Axon 2594

CAS [1380087-89-7]

MF C20H16ClN3O2
MW 365.81

Purity: 99%
Soluble in DMSO

CPI 0610

Description

Selective and metabolically stable inhibitor of the BET family of bromodomains (BET-BRD; IC50 values 0.12 - 0.17 μM and 0.22 μM for inhibition of BD-1 of BRD2-4 and BRDT, respectively), demonstrating a correlation between BET-driven reduction in MYC gene expression and tumor growth inhibition in a xenograft study. CPI 0610 displays essentially no activity in TR-FRET- or AlphaLisabased assays against the bromodomains of CBP, BRD9, BRPF1, PCAF, BRG1, ATAD2, TRIM24, BRD8 (IC50 value > 15 μM), and no meaningful inhibition in a CEREP express panel of about 50 GPCRs, ion channels, and transporters.

*Constellation Pharmaceuticals Inc compound; sold under agreement with Constellation Pharmaceuticals Inc.

BK Albrecht et al. Identification of a Benzoisoxazoloazepine Inhibitor (CPI-0610) of the Bromodomain and Extra-Terminal (BET) Family as a Candidate for Human Clinical Trials. J Med Chem. 2016 Feb 25;59(4):1330-9.

Certificate of Analysis
Material Safety Data Sheet

Apoptosis Cell Cycle Regulation Cell Signaling & Oncology Epigenetics BET (BRD)

Selective and metabolically stable inhibitor of BET bromodomains

Chemical name

2-((4S)-6-(4-chlorophenyl)-1-methyl-4H-benzo[e]isoxazolo[5,4-c]azepin-4-yl)acetamide

Source information

Constellation Pharmaceuticals Inc compound; sold under agreement with Constellation Pharmaceuticals Inc.

Parent CAS No.

[1380087-89-7]

產(chǎn)品資料

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