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TRIM24 and BRPF1 are potential therapeutic targets for cancer. Y08624 is a new TRIM24/BRPF1 dual inhibitor with reasonable Caco-2 permeability. Caco-2 permeability assay was performed by Medicilon

2023-07-17
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TRIM24 (tripartite motif-containing protein 24) and BRPF1 (bromodomain and PHD finger containing protein 1) are epigenetics “readers”and potential therapeutic targets for cancer and other diseases. Y08624 (Compound 20l) is a new TRIM24/BRPF1 dual inhibitor. Y08624 displays reasonable Caco-2 permeability. Caco-2 permeability assay was performed by Medicilon.

66.pngReference:

Qiuping Xiang, et al. Discovery, optimization and evaluation of 1-(indolin-1-yl)ethan-1-ones as novel selective TRIM24/BRPF1 bromodomain inhibitors. Eur J Med Chem. 2022 Jun 5;236:114311. doi: 10.1016/j.ejmech.2022.114311. 


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TAK-931 is a cancer therapeutic with a unique mechanism of action. Antitumor efficacy studies for TAK-931 were carried out at Medicilon
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Replication stress (RS) is a cancer hallmark; chemotherapeutic drugs targeting RS are widely used as treatments for various cancers. To develop next-generation RS-inducing anticancer drugs, cell division cycle 7 (CDC7) has attracted attention as a target. Researchers have developed an oral CDC7-selective inhibitor, TAK-931, as a candidate clinical anticancer drug. TAK-931 demonstrated marked, dose-dependent antitumor activity, without severe body weight loss. Antitumor efficacy studies for TAK-931 were carried out in two pancreatic PDX models, PHTX-249Pa and PHTXM-97Pa, at Medicilon.
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Address: 470 Wildwood Ave, Woburn, MA 01801 (America)

Tel: +1(626)986-9880(U.S.)

Address: Allia Future Business Centre Kings Hedges Road Cambridge CB4 2HY, UK

Tel: 0044 7790 816 954 (Europe)

Email: marketing@medicilon.com

  

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Fax: +86 (21) 5859-6369

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