Drug intelligence / Profile preview

Aurora A inhibitor I

Development stage
Unknown
Lead developer
Genentech
Modality
Small Molecules
Administration
Oral, Intravenous, Subcutaneous, Intraperitoneal, Parenteral, Implant, Topical, Rectal, Intranasal, Buccal, Vaginal
01

Overview

Aurora A inhibitor I (also known as TC-S 7010) is a potent, highly selective, ATP-competitive small molecule inhibitor of Aurora kinase A (AURKA) with an IC50 of 3.4 nM. Developed by Genentech, it exhibits approximately 1000-fold selectivity for Aurora kinase A over Aurora kinase B. The compound is widely used as a chemical biology tool to study mitotic spindle assembly, centrosome maturation, and cell cycle progression. In vitro, Aurora A inhibitor I induces G2/M cell cycle arrest and triggers apoptosis in various cancer cell lines, including colorectal carcinoma and leukemia cells.

Other names
Aurora A-IN-10Genentech Aurora A Inhibitor IGenentech Aurora Inhibitor IN-(2-chlorophenyl)-4-(2-(4-(2-(4-ethylpiperazin-1-yl)-2-oxoethyl)phenylamino)-5-fluoropyrimidin-4-ylamino)benzamide
02

Targets

AURKC (Aurora kinase C)AURKB (Aurora kinase B)AURKA (Aurora kinase A)

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