Contact Us marketing@medicilon.com
ABOUT
Company Profile
Corporate Culture
Management Team
Company History
Message from the CEO
Honors and Awards
SERVICES
SERVICES
01 Drug Discovery
Chemistry Research Biology Research Early Pharmacokinetics
02 Pharmaceutical Research
Intermediates Active Pharmaceutical Ingredients Pharmaceutical preparation Analytical Method Development and Quality Control CMC Filings Analytical Testing Center
03 Preclinical Research
Pharmacology & Pharmacodynamics Drug Safety Evaluation DMPK Bioanalysis IND Filings
PLATFORM
PLATFORM
01 One-stop Integrated Services
Liposome Drug Development Drug Discovery Pharmaceutical Research Preclinical Research Botanical Drug Preclinical R&D
02 Innovative Drug R&D Services
Peptide Drug Conjugate (PDC) Antibody Nucleic Acid Drug Cellular Immunotherapies mRNA Vaccine PROTAC ADC
03 Key Technical Services for Drug R&D
Cytokine and Biomarker Detection Metabolite Identification (MetID) Drug Forming Research Flow Cytometry Technology SEND Format Conversion Flow Sorting NanoString nCounter Detection Routes of Drug Administration
04 Drug Efficacy Evaluation for Common Diseases
Rodent Cerebrovascular Disease Inflammatory and Immune Diseases IO Pharmacodynamic Model
05 High-end Preparations Technology Platform
Skin Topical Preparation Ophthalmic drug Inhalation drug
06 Targeted Drugs R&D Services
STAT3-targeted Drugs R&D Service KRAS-targeted Drugs R&D Service GLP-1 New Drug R&D Service
07 Safety Assessment Lab of Process Chemistry

08 Public Services
CAREERS
Talent Development
Campus Recruitment
Recruitment
NEWS
Medicilon Events
Featured Stories
Market Events
Videos
A.C.E.
INVESTORS
Stock Information
Investment Contact
CLIENT CENTER
Intellectual Property Protection
Clients Testimonials
Downloads
Partnerships
Medicilon Support
Newsletters
CN
×
中
Message
Contact Us
Close Button
Back To Top
Online Message×
Click switch
Close Button
Customer Center
Customer Center
Case Studies Clients Testimonials Downloads Partnerships Intellectual Property Protection Newsletters
Home Client Center Publications

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
|
Page View：

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.

46.pngReference:

Qiuping Xiang, et al. Design, Synthesis, and Biological Evaluation of 1-(Indolizin-3-yl)ethan-1-ones as CBP Bromodomain Inhibitors for the Treatment of Prostate Cancer. J Med Chem. 2022 Jan 13;65(1):785-810. doi: 10.1021/acs.jmedchem.1c01864. 

Prostate-cancerCBP-bromodomainPharmacokineticLiver-microsomal-stability-assayCaco-2-permeability-assay
Share：
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.
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.
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.
Stock Code
688202

Global

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

Tel: +1(781)535-1428(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

Facebook icon
Twitter icon
Linkedin icon
Youtube icon
© 2023 Shanghai Medicilon Inc. All rights reserved All Rights Reserved Privacy Policy
Website Map
-->