Business Inquiry

Global：

Email:marketing@medicilon.com

+1(781)535-1428(U.S.)

0044 7790 816 954 (Europe)

China：

Email: marketing@medicilon.com.cn

Tel: +86 (21) 5859-1500

This site uses cookies and related technologies, as described in our privacy policy, for purposes that may include site operation, analytics, enhanced user experience, or advertising. You may choose to consent to our use of these technologies, or refuse these technologies

ARD-2128 is a PROTAC AR degrader with excellent plasma and microsomal stability. The in vitro stability and PK studies were performed by Medicilon

2023-07-11

Page View：

ARD-2128 is a bona fide PROTAC androgen receptor (AR) degrader and strongly suppresses AR-regulated genes in a dose- and time-dependent manner in AR+ prostate cancer cell lines. ARD-2128 has excellent plasma and microsomal stability in all the five species (Human, Mouse, Rat, Dog, and Monkey). The in vitro stability and pharmacokinetic (PK) studies were performed by Medicilon.

Reference:

Xin Han, et al. Strategies toward Discovery of Potent and Orally Bioavailable Proteolysis Targeting Chimera Degraders of Androgen Receptor for the Treatment of Prostate Cancer. J Med Chem. 2021 Sep 9;64(17):12831-12854. doi: 10.1021/acs.jmedchem.1c00882.

PROTAC androgen-receptor plasma-stability microsomal-stability pharmacokinetic

Return

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.

Design, synthesis, and biological evaluation of CBP bromodomain inhibitors for the treatment of prostate cancer. PK evaluation, liver microsomal stability assay, and Caco-2 permeability assay were performed at Medicilon

2023-07-11

Prostate cancer (PCa) is one of the most commonly diagnosed cancers and the leading cause of cancer mortalities in men. CREB (cyclic-AMP responsive element binding protein) binding protein (CBP) is a potential target for prostate cancer treatment. Researchers designed 1-(Indolizin-3-yl)ethan-1-ones as CBP bromodomain inhibitors for the treatment of prostate cancer. Pharmacokinetic properties evaluation were analyzed by Medicilon. Liver microsomal stability assay were performed at Medicilon. Caco-2 permeability assay was analyzed by Medicilon.

SLL-1206 is a kappa opioid receptor agonist with substantially improved physicochemical and pharmacokinetic properties

2023-07-11

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.