PF-2771

PF-2771 is a potent and selective centromere protein E (CENP-E) inhibitor, inhibiting CENP-E motor activity with an IC₅₀ of 16.1 nM; PF-2771 is used as an anticancer agent. IC50 & Target: IC50: 16.1 nM (CENP-E)^[1] In Vitro: PF-2771 is a potent and selective CENP-E inhibitor, inhibiting CENP-E motor activity with an IC₅₀ of 16.1 nM. PF-2771 shows no inhibitory effect on the ATPase activities of highly related kinesins (0% inhibition of Eg5/KSP, chromokinesin, and MCAK at both 1 or 10 μM PF-2771). PF-2771 exhibits inactive activity against 74 protein kinases (all < 23% inhibition with 1 μM PF-2771, < 40% with 10 μM PF-2771). PF-2771 is cytotoxic to the basal-like breast cancer tumor cell survival, with EC₅₀s of < 0.1 μM, and with no cytotoxicity on the normal and premalignant cell lines (EC₅₀ > 5 μM). PF-2771 (100 nM) reusults in a chromosomal congression defect in MDA-MB-468 cells^[1]. In Vivo: PF-2771 (100 mg/kg, every day i.p.) potently inhibits CENP-E motor function, and causes tumor regression in SCID mice bearing AA1077 mammary tumors^[1].