PF-2771 是一种选择性的着丝粒蛋白 E (CENP-E) 抑制剂，IC₅₀ 值为 16.1 nM，具有抗肿瘤活性。

PF-2771 is a potent and selective centromere protein E (CENP-E) inhibitor, inhibiting CENP-E motor activity with an IC 50 of 16.1 nM; PF-2771 is used as an anticancer agent.

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CENP-E 16.1 nM (IC50)

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. has not independently confirmed the accuracy of these methods. They are for reference only.

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. has not independently confirmed the accuracy of these methods. They are for reference only.

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Powder -20°C 3 years；4°C 2 years

[1]. Kung PP, et al. Chemogenetic evaluation of the mitotic kinesin CENP-E reveals a critical role in triple-negative breast cancer. Mol Cancer Ther. 2014 Aug;13(8):2104-15.

In Vitro: DMSO : ≥ 32 mg/mL (57.75 mM)配制储备液