- ¥500
- 喀露蓝
- 上海
- CPDB1974
- 2025年06月28日
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- 详细信息
- 技术资料
- 保质期：
2年
- 英文名：
5-[6-(4-Methyl-piperazin-1-ylmethyl)-benzoimidazol-1-yl]-3-[1-(2-trifluoromethyl-phenyl)-ethoxy]-thiophene-2-carboxylic acid amide
- 库存：
现货 100mg-100g
- 供应商：
喀露蓝
- 规格：
98% min
GSK461364 is a potent small molecule Polo-like kinase 1 (PLK1) inhibitor with a Ki of 2.2 nM. IC50 Value: 2.2 nM(Ki) Target: PLK1 in vitro: GSK461364 is a potent inhibitor of cell proliferation causing 50% growth inhibition (GI50) below 100 nM in most of the cell lines tested with limited toxicity against human nonproliferating cells. Inhibition of cell cycle progression is concentration dependent with initial delay at G2 phase at high GSK461364 concentrations and arrest at M phase at lower concentrations. Currently, GSK461364 is in a dose-escalation first-time-in-human trial. Cell lines with mutations in the TP53 gene tended to be more sensitive to GSK461364, and that inhibiting the p53 response by RNA silencing confers increased sensitivity in some p53 wild-type (WT) cells. Furthermore, these more sensitive cell lines also have increased levels of chromosome instability, a characteristic associated with TP53 mutations. In preclinical testing, GSK461364 shows antiproliferative activity against multiple (>120) tumor cell lines and potently inhibits the proliferation of greater than 83% and 91% of these cell lines, with IC50 values lower than 50 and 100 nM, respectively. in vivo: GSK461364 shows a dose-dependent mitotic arrest in mouse xenografts, which correlates with effects on tumor growth. Intraperitoneal administration of GSK461364 causes regression or tumor growth delay in different xenograft models, including Colo205 xenografts. Suppression of Plk1 in vivo by using GSK461364 results in mitotic arrest with aberrant mitotic figures consisting of monopolar or collapsed mitotic spindles.
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公司优势：有新药开发能力，生物活性筛选及药物代谢动力学研究，有从实验室到工厂放大合成经验，专业书写各种需求资料，可以提供FTE实验室，有专业增值服务，价格低等优势。
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GSK-461364
¥500
