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PARP1/2 inhibitors are the promising candidate for the treatment of cancer. The PARP1/2 inhibition assays were performed by Medicilon

2023-07-11
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Poly ADP-ribose polymerases (PARPs) are a family of enzymes related to DNA damage repair process. 

Inhibition of PARP1/2 accelerates the damage of injured DNA, which is synthetically lethal to DNA-repairing-deficient cancer cells, such as BRCA1/2-deficient cells. 

PARP1/2 inhibitors could be a promising candidate for the treatment of cancer.

The PARP1 and PARP2 inhibition assays were performed by Medicilon. 

57.jpgReference:

Lin Tang, et al. Discovery of the PARP (poly ADP-ribose polymerase) inhibitor 2-(1-(4,4-difluorocyclohexyl)piperidin-4-yl)-1H-benzo[d]imidazole-4-carboxamide for the treatment of cancer. Bioorg Chem. 2021 Sep;114:105026. doi: 10.1016/j.bioorg.2021.105026. 

PARPDNA-damage-repairinhibition-assay
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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
2023-08-21
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.
Design, synthesis, and biological evaluation of potent PPARα/δ dual agonists for the treatment of nonalcoholic steatohepatitis. The PK studies, hERG studies, and Ames tests were conducted by Medicilon
2023-07-11
Nonalcoholic steatohepatitis (NASH) is the advanced subtype of nonalcoholic fatty liver disease (NAFLD) and is becoming a severe global public health problem. PPARα/δ are regarded as potential therapeutic targets for NASH. Herein, researchers report a series of novel triazolone derivatives as PPARα/δ dual agonists. The pharmacokinetic studies were conducted by Medicilon. The hERG channel inhibition studies were conducted by Medicilon. The Ames tests were conducted by Medicilon.
Discovery and synthesis of a new class of selective TNIK inhibitors and evaluation of their anti-colorectal cancer effects, the pharmacokinetic properties was carried out by Medicilon
2023-07-11
The Traf2- and Nck-interacting protein kinase (TNIK) is a downstream signal protein of the Wnt/β-catenin pathway and has been thought of as a potential target for the treatment of colorectal cancer. SAR analysis leads to the identification of a number of potent TNIK inhibitors with Compound 21k being the most active one. Preliminary assessment for the pharmacokinetic properties of Compound 21k was carried out through services provided by Medicilon.
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688202

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Address: 20 Maguire Road, Suite 103, Lexington, MA 02421(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

  

Address: 5th Floor, 62, Banpodae-ro 4-gil, Seocho-gu, Seoul, 06719 South Korea

Tel: +82 70-8269-5849

China

Address: No.585 Chuanda Road, Pudong New Area, Shanghai (Headquarters)

Postcode: 201299

Tel: +86 (21) 5859-1500 (main line)

Fax: +86 (21) 5859-6369

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