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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。
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。
规格 | 价格 | 库存 | 数量 |
---|---|---|---|
100 mg | ¥ 14,218 | 6-8周 |
产品描述 | PF-2771 is a potent and selective centromere protein E (CENP-E) inhibitor. PF-2771 inhibits CENP-E motor activity with an IC 50 of 16.1 nM. PF-2771 is used as an anticancer agent. |
靶点活性 | CENP-E:16.1 nM |
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]. |
分子量 | 554.08 |
分子式 | C29H36ClN5O4 |
CAS No. | 2070009-55-9 |
存储 | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice. | ||||||||||||||||||||||||||||||
溶解度信息 | DMSO: 32 mg/mL (57.75 mM) | ||||||||||||||||||||||||||||||
溶液配制表 | |||||||||||||||||||||||||||||||
DMSO
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