Drug intelligence / Profile preview

Compound 59

Development stage
Preclinical
Lead developer
Nerviano Medical Sciences
Modality
Small Molecules
Administration
Oral
01

Overview

Compound 59 is a potent, orally bioavailable small molecule inhibitor of multiple cyclin-dependent kinases (CDKs), belonging to the pyrazolo[4,3-h]quinazoline-3-carboxamide chemical class. Developed by Nerviano Medical Sciences, it was identified through the optimization of a pyrazolo-quinazoline scaffold to improve solubility, pharmacokinetic properties, and inhibitory activity against tumor cells compared to earlier hit compounds like Compound 1. In preclinical studies, Compound 59 demonstrated significant in vivo efficacy in ovarian carcinoma xenograft models, such as A2780, by inducing cell cycle arrest and inhibiting CDK-mediated signaling pathways. The compound is designed to target the dysregulated cell cycle progression that is a hallmark of most cancer cells, making it a potential antineoplastic agent.

Other names
8-[4-(4-methylpiperazine-1-carbonyl)phenylamino]-1-methyl-4,5-dihydro-1H-pyrazolo[4,3-h]quinazoline-3-carboxamideNerviano Compound 59
02

Targets

CDK1 (Cyclin-dependent kinase 1)CDK5 (Cyclin-dependent kinase 5)CDK4 (Cyclin-dependent kinase 4)CDK2 (Cyclin-dependent kinase 2)

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