Drug intelligence / Profile preview

AS-10

Development stage
Preclinical
Lead developer
Penn State College of Medicine
Modality
Small Molecules
01

Overview

AS-10 is a novel organoselenium small molecule developed by researchers at the Penn State College of Medicine as a potential therapeutic for pancreatic and colorectal cancers. Identified through structure-activity relationship (SAR) studies, AS-10 functions as a multi-targeted agent that inhibits the NF-κB inflammatory pathway and acts as an acetyl donor for histone acetyltransferase (HAT). By inducing HAT activity, AS-10 promotes histone acetylation and subsequent gene expression changes that lead to G1 and G2 cell cycle arrest and apoptosis. Preclinical studies have demonstrated its efficacy against various cancer cell lines, including those resistant to standard FOLFOX therapy, and its ability to significantly reduce tumor growth in HCT116 xenograft models with minimal systemic toxicity. Additionally, AS-10 has shown synergistic potential when combined with gemcitabine in pancreatic cancer models.

02

Targets

KAT2BNF-κB

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