Drug intelligence / Profile preview

SKLB163

Development stage
Preclinical
Lead developer
Collaborative Innovation Center of Biotherapy
Modality
Small Molecules
Administration
Oral
01

Overview

SKLB163 is a small molecule antitumor agent developed by the Collaborative Innovation Center of Biotherapy (State Key Laboratory of Biotherapy) at Sichuan University. It is characterized as a multi-target inhibitor, primarily acting as a tubulin polymerization inhibitor by binding to the colchicine-binding site, which leads to G2/M phase cell cycle arrest and apoptosis. Additionally, research and patents associated with the compound indicate its role as an inhibitor of the MDM2-p53 protein-protein interaction, a mechanism that restores the activity of the p53 tumor suppressor protein. SKLB163 has demonstrated potent in vitro and in vivo efficacy against various cancer types, including those with multi-drug resistance, and is currently in the preclinical pipeline for cancer therapy.

02

Targets

AKT (RAC-alpha serine/threonine-protein kinase)CASP3 (Caspase-3)ERK1/2 (Mitogen-activated protein kinase 1/3 (ERK2/ERK1))RhoGDI1 (RhoGDI1 / ARHGDIA)JNK (Mitogen-activated protein kinase kinase kinase family)

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