Delving into the Latest Updates on D-181 with Synapse

Overview

Basic Info

Drug Type

Small molecule drug

Synonyms

Target

FGFR1 x FLT3 x PDGFRβ x Tubulin x VEGFR x c-Kit

Mechanism

FGFR1 antagonists(Fibroblast growth factor receptor 1 antagonists), FLT3 inhibitors(Tyrosine-protein kinase receptor FLT3 inhibitors), PDGFRβ inhibitors(Platelet-derived growth factor receptor beta inhibitors)

+ [3]

Therapeutic Areas

Neoplasms

Active Indication-

Inactive Indication

Neoplasms

Originator Organization

Gibh

Active Organization-

Inactive Organization

Gibh

East China University of Science & Technology

Drug Highest PhasePendingDiscovery

First Approval Date-

Regulation-

Receptor tyrosine kinases (RTKs) modulate a variety of cellular events, including cell proliferation, differentiation, mobility and apoptosis. In addition, RTKs have been validated as targets for cancer therapies. Microtubules are another class of proven targets for many clinical anticancer drugs. Here, we report that 1-(4-chloro-3-(trifluoromethyl) phenyl)-3-(2-cyano-4-hydroxyphenyl)urea (D181) functions as both a receptor tyrosine kinase inhibitor and a tubulin polymerization enhancer. D181 displayed potent inhibitory activities against a panel of RTKs, including Flt3, VEGFR, cKit, FGFR1 and PDGFRβ. D181 also enhanced tubulin polymerization and modified the secondary structure of tubulin proteins to disrupt their dynamic instability. Because of synergistic cooperation, D181 strongly inhibited the proliferation of various cancer cell lines, induced LoVo cell cycle arrest in the G1 and M phases and suppressed tumor growth in nude mice bearing human LoVo and HT29 xenografts. Our studies have provided a new, promising lead compound and novel clues for multi-target anticancer drug design and development.

100 Deals associated with D-181

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