化合物 T12434 T12434

Product Introduction
Bioactivity


英文名: PF-2771

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

体外活性: PF-2771 is a potent and selective CENP-E inhibitor, inhibiting CENP-E motor activity with an IC 50 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 EC 50 s of < 0.1 μM, and with no cytotoxicity on the normal and premalignant cell lines (EC 50 > 5 μM). PF-2771 (100 nM) causes a chromosomal congression defect in MDA-MB-468 cells [1].

体内活性: PF-2771 (100 mg/kg, every day i.p.) potently inhibits CENP-E motor function, and leads to tumor regression in SCID mice bearing AA1077 mammary tumors [1].

存储条件: Powder: -20°C for 3 years | In solvent: -80°C for 1 year

溶解度: DMSO : 32 mg/mL (57.75 mM)


关键字: PF 2771 | PF2771 | PF-2771

相关产品: Paprotrain | NMS-P715 | BOS-172722 | Empesertib | Monastrol | (S)-Monastrol | PVZB1194 | Dimethylenastron | Mps1-IN-2 | EMD534085

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注：该产品未在中华人民共和国食品药品监督管理部门申请医疗器械注册和备案，不可用于临床诊断或治疗等相关用途