TC-A 2317 hydrochloride

TC-A 2317 hydrochloride is an orally active Aurora A kinase inhibitor (Ki=1.2 nM). TC-A 2317 hydrochloride exhibits excellent selectivity to Aurora B kinase (Ki=101 nM) and other 60 kinases, good cell permeability and good PK profile. Antitumor activity[1].

Signaling Pathways >> Epigenetics >> Aurora Kinase

Research Areas >> Cancer

Signaling Pathways >> Cell Cycle/DNA Damage >> Aurora Kinase

Aurora A:1.2 nM (Ki)

Aurora B:101 nM (Ki)

TC-A 2317 hydrochloride (Compound 6) inhibits proliferation of HCT116 cells with an IC50 of 115 nM[1].

TC-A 2317 hydrochloride is effective in antitumor mice model without decrease of body weight[1]. TC-A 2317 hydrochloride shows good PK profile; Cmax value is 4930 nM (Tmax=1.2 h) and serum concentration after 24 h is 52 nM (T1/2=3.3 h) at 30 mg/kg po in rats[1]. Animal Model: HCT-116 Xenograft mice mode[1] Dosage: P.o.; daily for 14 days Administration: 30 mg/kg Result: Growth of tumor was inhibited by 59% after 14 days.

[1]. Ando R, et al. 3-Cyano-6-(5-methyl-3-pyrazoloamino)pyridines: selective Aurora A kinase inhibitors. Bioorg Med Chem Lett. 2010;20(15):4709-4711.