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PF-2771
CAS No. : 2070009-55-9
MCE 国际站:PF-2771
产品活性: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。
研究领域:Cell Cycle/DNA Damage | Cytoskeleton
作用靶点:Kinesin
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.
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.
相关产品:Bioactive Compound Library Plus | Cell Cycle/DNA Damage Compound Library | Anti-Cancer Compound Library | Anti-Aging Compound Library | Cytoskeleton Compound Library | Anti-Breast Cancer Compound Library | Targeted Diversity Library | Pain-Related Compound Library | Highly Selective Inhibitors Library | Bioactive Compound Library Max | Ispinesib | Filanesib | GSK-923295 | Monastrol | AZ82 | SB-743921 hydrochloride | Litronesib | S-Trityl-L-cysteine | Paprotrain | Dimethylenastron | EMD534085 | GW406108X | Kif15-IN-1 | CW-069 | PVZB1194 | ARQ 621 | BRD9876 | K858 (Racemic) | Kif15-IN-2 | AZD4877 | Eg5 Inhibitor V, trans-24 | MK-0731 | MC-Val-Cit-PAB-Ispinesib | Anticancer agent 190 | CENP-E-IN-2 | CENP-E-IN-3 | Eg5-IN-1
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