Delving into the Latest Updates on YW-2065 with Synapse

Overview

Basic Info

Drug Type

Small molecule drug

Synonyms

Pyrazole-4-Carboxamide

Target

AMPK x AXIN1

Mechanism

AMPK agonists(AMP activated protein kinase agonists), AXIN1 stimulants(axin 1 stimulants)

Therapeutic Areas

NeoplasmsDigestive System Disorders

Active Indication

Colorectal Cancer

Inactive Indication-

Originator Organization

University of Maryland Baltimore

Active Organization

University of Maryland Baltimore

Inactive Organization-

Drug Highest PhasePreclinical

First Approval Date-

Regulation-

Structure

Molecular FormulaC20H15BrN4O

InChIKeyATYUYECWVYSPBS-UHFFFAOYSA-N

CAS Registry2131223-85-1

Dysregulation of the Wnt/β-catenin signaling pathway has been widely recognized as a pathogenic mechanism for colorectal cancer (CRC). Although numerous Wnt inhibitors have been developed, they commonly suffer from toxicity and unintended effects. Moreover, concerns have been raised in targeting this pathway because of its critical roles in maintaining stem cells and regenerating tissues and organs. On the basis of the anthelmintic drug pyrvinium and previous lead FX1128, we have developed a compound YW2065 (1c) which demonstrated excellent anti-CRC effects in vitro and in vivo. YW2065 achieves its inhibitory activity for Wnt signaling by stabilizing Axin-1, a scaffolding protein that regulates proteasome degradation of β-catenin. Simultaneously, YW2065 also led to the activation of the tumor suppressor AMPK, providing an additional anticancer mechanism. In addition, YW2065 showed favorable pharmacokinetic properties without obvious toxicity. The anti-CRC effect of YW2065 was highlighted by its promising efficacy in a mice xenograft model.

100 Deals associated with YW-2065

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