化合物 T12434

CAS号:2070009-55-9
英文名: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)-
中文名:化合物 T12434
CBNumber:CB38252174
分子式:C29H36ClN5O4
分子量:554.08
MOL File:2070009-55-9.mol

化合物 T12434化学性质

化合物 T12434性质、用途与生产工艺

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.

化合物 T12434上下游产品信息

上游原料

下游产品

化合物 T12434生产厂家