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Researchers successfully discovered an orally available PROTAC degrader SIAIS164018 with orally bioavailable and well tolerated in vivo. PK and MTD assays were performed by Medicilon

2023-07-11
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PROTAC is an attractive technology in drug discovery. Researchers successfully discovered an orally available PROTAC degrader SIAIS164018 which degrades not only ALK or mutant EGFR but also oncoproteins involved in metastasis. SIAIS164018 is orally bioavailable and well tolerated in vivo. Pharmacokinetic and maximal tolerated dose (MTD) assays were performed by Medicilon.

59.pngReference:

Chaowei Ren, et al. Discovery of a Brigatinib Degrader SIAIS164018 with Destroying Metastasis-Related Oncoproteins and a Reshuffling Kinome Profile. J Med Chem. 2021 Jul 8;64(13):9152-9165. doi: 10.1021/acs.jmedchem.1c00373. 


PROTACdrug-discoveryPharmacokineticmaximal-tolerated-dose
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Relevant News
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.
SLL-1206 is a kappa opioid receptor agonist with substantially improved physicochemical and pharmacokinetic properties
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The search for selective kappa opioid receptor (κOR) agonists with an improved safety profile is an area of interest in opioid research. SLL-1206 is a κOR agonist with single-digit nanomolar activities. SLL-1206 exhibits substantially improved physicochemical and pharmacokinetic properties, and reduces central nervous system effects. The authors are grateful to Medicilon Preclinical Research LLC. for pharmacokinetic studies on SLL-1206.
ARD-2585 is an orally active PROTAC degrader of androgen receptor for the treatment of advanced prostate cancer
2023-07-11
A PROTAC-based androgen receptor (AR) degrader is a bifunctional small molecule, consisting of an AR ligand that binds to AR protein, and a ligand that binds to and recruits an E3 ligase complex, tethered together through a linker. Researchers report the discovery of exceptionally potent and orally bioavailable PROTAC AR degrader ARD-2585 (Compound 43). ARD-2585 is a promising AR degrader for extensive investigations for the treatment of advanced prostate cancer. The liver microsomal stability assay was performed by Medicilon. The plasma stability assay was performed by Medicilon. The hERG assay was performed by Medicilon.
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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

  

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Fax: +86 (21) 5859-6369

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