1137212-79-3

Plogosertib (CYC140) is a selective, potent, and orally active ATP-competitive PLK1 inhibitor (IC50: 3 nM). Plogosertib is an anti-cancer agent with anti-proliferative activity. Plogosertib can be used in the research of several tumors, including esophageal, gastric, leukemia, non–small cell lung cancer, ovarian, and squamous cell cancers[1][2].

PLK1: 3 nM (IC₅₀); PLK2: 149 nM (IC₅₀); PLK3: 393 nM (IC₅₀)

[1] Sylvie Moureau, et al. Abstract 4178: The novel PLK1 inhibitor, CYC140: Identification of pharmacodynamic markers, sensitive target indications and potential combinations. Cancer Res (2017) 77 (13_Supplement): 4178.
[2] Moureau S, et al. Therapeutic potential of novel PLK1 inhibitor CYC140 in esophageal cancer and acute leukemia[J]. European Journal of Cancer, 2016, 1(69): S117.
[3] Susan Davis, et al. Treatment of proliferative diseases with pyrimidodiazepinones. Patent US20150320762A1.