Delving into the Latest Updates on KY1022 with Synapse

Overview

Basic Info

Drug Type

Small molecule drug

Synonyms

Target

CTNNB x RAS

Mechanism

CTNNB inhibitors(Beta catenins inhibitors), RAS inhibitors(RAS type GTPase family inhibitors)

Therapeutic Areas

NeoplasmsDigestive System Disorders

Active Indication

Colorectal Cancer

Inactive Indication-

Originator Organization

Yonsei University

Active Organization

Yonsei University

Inactive Organization-

Drug Highest PhasePreclinical

First Approval Date-

Regulation-

Structure

Molecular FormulaC17H19N3OS

InChIKeyINRQXFWQQLFWNZ-UHFFFAOYSA-N

CAS Registry1029721-36-5

APC (80-90%) and K-Ras (40-50%) mutations frequently occur in human colorectal cancer (CRC) and these mutations cooperatively accelerate tumorigenesis including metastasis. In addition, both β-catenin and Ras levels are highly increased in CRC, especially in metastatic CRC (mCRC). Therefore, targeting both the Wnt/β-catenin and Ras pathways could be an ideal therapeutic approach for treating mCRC patients. In this study, we characterized the roles of KY1022, a small molecule that destabilizes both β-catenin and Ras via targeting the Wnt/β-catenin pathway, in inhibiting the cellular events, including EMT, an initial process of metastasis, and apoptosis. As shown by in vitro and in vivo studies using APCMin/+/K-RasG12DLA2 mice, KY1022 effectively suppressed the development of mCRC at an early stage of tumorigenesis. A small molecular approach degrading both β-catenin and Ras via inhibition of the Wnt/β-catenin signaling would be an ideal strategy for treatment of mCRC.

100 Deals associated with KY1022

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