GSK-461364 is a Polo-like kinase 1 inhibitor, is also a small molecule Polo-like kinase 1 (PLK1) inhibitor with potential antineoplastic activity. Polo-like kinase 1 inhibitor GSK461364 selectively inhibits Plk1, inducing selective G2/M arrest followed by apoptosis in a variety of tumor cells while causing reversible cell arrest at the G1 and G2 stage without apoptosis in normal cells. Plk1, named after the polo gene of Drosophila melanogaster, is a serine/threonine protein kinase involved in regulating mitotic spindle function in a non-ATP competitive manner.
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化学信息
名称 | GSK-461364 |
Iupac 化学名称 | (R)-5-(6-((4-methylpiperazin-1-yl)methyl)-1H-benzo[d]imidazol-1-yl)-3-(1-(2-(trifluoromethyl)phenyl)ethoxy)thiophene-2-carboxamide |
同义词 | GSK461364; GSK 461364 |
英文同义词 | GSK461364; GSK 461364 |
分子式 | C27H28F3N5O2S |
分子量 | 543.60373 |
Smile | CN1CCN(CC1)CC=1C=CC2=C(N(C=N2)C2=CC(=C(S2)C(=O)N)O[C@H](C)C2=C(C=CC=C2)C(F)(F)F)C1 |
InChiKey | ZHJGWYRLJUCMRT-QGZVFWFLSA-N |
InChi | InChI=1S/C27H28F3N5O2S/c1-17(19-5-3-4-6-20(19)27(28,29)30)37-23-14-24(38-25(23)26(31)36)35-16-32-21-8-7-18(13-22(21)35)15-34-11-9-33(2)10-12-34/h3-8,13-14,16-17H,9-12,15H2,1-2H3,(H2,31,36)/t17-/m1/s1 |
Cas号 | 929095-18-1 |
相关CAS号 | |
外观性状 | Solid powder |
纯度 | 98% by HPLC |
存储 | -20 ºC for 3 years |
可溶性 | Soluble in DMSO |
处理方式 | |
运输条件 | Shipped under ambient temperature |
海关编码 | |
Targets | |
Mechanism | |
Cell study | |
Animal study | |
Clinical study | |