Drug intelligence / Profile preview

compound 12b

Development stage
Preclinical
Modality
Small Molecules
Administration
Oral
01

Overview

"Compound 12b" is a designation used for multiple distinct experimental small molecule candidates in preclinical oncology research. One version is a novel, potent, and orally available covalent dual inhibitor of Cyclin-dependent kinase 12 (CDK12) and Cyclin-dependent kinase 13 (CDK13). This compound exhibits robust in vivo antitumor properties by targeting these kinases, which are essential for transcriptional regulation and DNA damage response. A separate chemical entity also referred to as "compound 12b" is a benzimidazolone-bridged hybrid molecule featuring a coumarin substituent. This hybrid compound has demonstrated significant antiproliferative activity and selectivity against human cervical (HeLa), breast (MCF-7), and lung (A549) cancer cell lines in vitro, with molecular docking studies suggesting potential affinity for Vascular endothelial growth factor receptor 2 (VEGFR2) and Cyclin-dependent kinase 4 (CDK4).

02

Targets

CDK13

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