Drug intelligence / Profile preview

CYC116

Development stage
Phase 1
Lead developer
Cyclacel Pharmaceuticals
Modality
Small Molecules
Administration
Oral
01

Overview

CYC116 is an orally bioavailable, small molecule multi-kinase inhibitor developed as an anticancer agent. Its primary mechanism of action is the inhibition of Aurora kinase A and Aurora kinase B, which are serine/threonine protein kinases essential for cell division. By inhibiting these kinases, CYC116 disrupts the cell cycle and induces apoptosis in cancer cells. Additionally, it inhibits vascular endothelial growth factor receptor 2 (VEGFR2), thereby impeding angiogenesis required for tumor growth. Preclinical studies have shown antitumor activity in both solid tumors and hematological cancers. The drug has also demonstrated effects on mast cells by inhibiting Fyn kinase, leading to reduced degranulation and cytokine release, suggesting potential utility beyond oncology[1][2][3][6].

Other names
4-methyl-5-(2-(4-morpholinophenylamino)pyrimidin-4-yl)thiazol-2-amine693228-63-6
02

Targets

FYN (Proto-oncogene tyrosine-protein kinase Fyn)AURKA (Aurora kinase A)VEGFR2 (Vascular endothelial growth factor receptor 2)AURKB (Aurora kinase B)

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