化合物 T12434
化合物 T12434 性质
| 密度 | 1.22±0.1 g/cm3(Predicted) |
|---|---|
| 储存条件 | Store at -20°C |
| 溶解度 | 二甲基亚砜：≥32mg/mL（57.75mM） |
| 形态 | 固体 |
| 酸度系数(pKa) | 13.32±0.46(Predicted) |
| 颜色 | 白色至米白色 |
化合物 T12434 用途与合成方法
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CENP-E 16.1 nM (IC 50 ) |
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) reusults in a chromosomal congression defect in MDA-MB-468 cells.
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.
