2070009-55-9

中文名称化合物 T12434

英文名称 Benzamide, N-[(1S)-2-[4-(2-acetyl-1-methyl-1H-imidazol-4-yl)phenyl]-1-[[[2-(dimethylamino)acetyl]amino]methyl]ethyl]-3-chloro-4-(1-methylethoxy)-

CAS 2070009-55-9

分子式 C29H36ClN5O4

分子量 554.08

MOL 文件 2070009-55-9.mol

2070009-55-9 结构式

基本信息物理化学性质常见问题列表

基本信息

中文别名

化合物 T12434

英文别名

Benzamide, N-[(1S)-2-[4-(2-acetyl-1-methyl-1H-imidazol-4-yl)phenyl]-1-[[[2-(dimethylamino)acetyl]amino]methyl]ethyl]-3-chloro-4-(1-methylethoxy)-

物理化学性质

密度1.22±0.1 g/cm3(Predicted)

储存条件-20°C储存

溶解度DMSO : ≥ 32 mg/mL (57.75 mM)

酸度系数(pKa)13.32±0.46(Predicted)

形态Solid

颜色White to off-white

常见问题列表

生物活性

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。

靶点

CENP-E

16.1 nM (IC ₅₀ )

体外研究

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.

体内研究

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.