Drug intelligence / Profile preview

AGN193198

Development stage
Unknown
Lead developer
Allergan
Modality
Small Molecules
Administration
Oral
01

Overview

AGN193198 is a novel retinoid-related small molecule developed by Allergan. Although structurally similar to retinoids, it operates through a mechanism independent of the classical retinoic acid receptors (RAR) and retinoid X receptors (RXR). Research in pancreatic cancer models demonstrates that AGN193198 inhibits cell proliferation more effectively than high-affinity receptor-selective retinoids. Its mechanism of action involves inducing G2/M phase cell cycle arrest by suppressing the expression and activity of key regulatory proteins, including Cyclin A, Cyclin B1, Cyclin D1, Cyclin E, and cyclin-dependent kinases (CDK1, CDK2, and CDK4), while simultaneously upregulating the inhibitors p21 and p27. Furthermore, it triggers apoptosis via the activation of caspases 3, 8, and 9.

Other names
4-[3-(1-heptyl-4,4-dimethyl-2-oxo-1,2,3,4-tetrahydroquinolin-6-yl)-3-oxo-propenyl] benzoic acid
02

Targets

CASP9 (Caspase-9)CDK2 (Cyclin-dependent kinase 2)CASP3 (Caspase-3)CASP8 (Caspase-8)

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