Drug intelligence / Profile preview

Chinese Academy of Sciences CDK9 compound 29

Development stage
Preclinical
Lead developer
Chinese Academy of Sciences
Modality
PROTACs (E3 ligase recruitment) → Targeted Protein Degraders (TPDs) → Small Molecules
01

Overview

Chinese Academy of Sciences CDK9 compound 29: sourced facts only. name: "The developed compound 29 exhibited a desired potency (DC50 = 3.94 nM) with high efficacy (Dmax = 96 %) on CDK9 degradation, and effectively inhibited the proliferation of TNBC MDA-MB-231 cells." [PMID:39406109]; target: "The developed compound 29 exhibited a desired potency (DC50 = 3.94 nM) with high efficacy (Dmax = 96 %) on CDK9 degradation, and effectively inhibited the proliferation of TNBC MDA-MB-231 cells." [PMID:39406109]; developer: "School of Pharmaceutical Science and Technology, Hangzhou Institute for Advanced Study, University of Chinese Academy of Sciences, Hangzhou, China; State Key Laboratory of Drug Research, Shanghai Institute of Materia Medica, Chinese Academy of Sciences, Shanghai 201203, China." [PMID:39406109]; modality: "We herein present the design, synthesis, and extensive biological evaluation of a series of novel PROTACs as orally bioavailable, potent and selective degraders of CDK9 for targeting transcription regulation in triple-negative breast cancer." [PMID:39406109]; stage: "oral administration of degrader 29 significantly depleted CDK9 protein in TNBC tumor tissues and exhibited tumor growth inhibition in TNBC xenograft mice models." [PMID:39406109]

02

Targets

CDK9 (Cyclin-dependent kinase 9)

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