Drug intelligence / Profile preview

ON 108600

Development stage
Preclinical
Lead developer
Traws Pharma
Modality
Small Molecules
Administration
Intraperitoneal
01

Overview

ON 108600 is a novel, preclinical-stage small molecule multi-kinase inhibitor that simultaneously targets casein kinase 2 (CK2), TRAF2- and NCK-interacting kinase (TNIK), and dual-specificity tyrosine-phosphorylation-regulated kinase (DYRK) family kinases. Developed by Traws Pharma (formerly Onconova Therapeutics) in collaboration with the Icahn School of Medicine at Mount Sinai, ON 108600 is designed to target breast cancer stem cell-like cells (BCSCs) and overcome chemotherapy resistance in triple-negative breast cancer (TNBC). By simultaneously inhibiting CK2, TNIK, and DYRK1, the compound induces G2/M cell cycle arrest and apoptosis in TNBC cells and cancer stem cells. Preclinical studies have demonstrated its efficacy in suppressing tumor growth and brain metastases in animal models of TNBC, both as a monotherapy and in combination with chemotherapy.

Other names
(E)-6-((2,6-dichlorobenzyl)sulfonyl)-2-(4-hydroxy-3-nitrobenzylidene)-2H-benzo[b][1,4]thiazin-3-ol
02

Targets

AKT1 (Proto-oncogene serine/threonine-protein kinase Akt1)CCND1 (Cyclin D1)CDKN1B (Transmembrane emp24 domain-containing protein 7)CK2 (Casein kinase II subunit alpha)CSNK2A2 (Casein kinase II subunit alpha prime)DYRK1A (Dual-specificity tyrosine-phosphorylation-regulated kinase 1A)DYRK1B (Dual specificity tyrosine-phosphorylation-regulated kinase 1B)DYRK2 (Dual-specificity tyrosine-phosphorylation-regulated kinase 2)TNIK (TRAF2- and NCK-interacting kinase)

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