S82078 |
TAK-960 |
源葉(MedMol) | 99% |
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- 產(chǎn)品描述: TAK-960 is an orally available, selective inhibitor of polo-like kinase 1 (PLK1), with an IC50 of 0.8 nM. TAK-960 also shows inhibitory activities against PLK2 and PLK3, with IC50s of 16.9 and 50.2 nM, respectively. TAK-960 inhibits proliferation of multiple cancer cell lines and exhibits significant efficacy against multiple tumor xenografts
- 靶點(diǎn): PLK1:0.8 nM (IC50);PLK2:16.9 nM (IC50);PLK3:50.2 nM (IC50);FAK/PTK2:19.6 nM (IC50);MLCK/MYLK:25.6 nM (IC50);FES/FPS:58.2 nM (IC50);PLK
- 體內(nèi)研究:
TAK-960 exhibits (10 mg/kg; p.o.; once daily for 2 weeks) significant efficacy against multiple tumor xenografts. In animal models, TAK-960 (p.o.) increases pHH3 in a dose-dependent manner and significantly inhibits the growth of HT-29 colorectal cancer xenografts
- 參考文獻(xiàn):
1. Hikichi Y, et al. TAK-960, a novel, orally available, selective inhibitor of polo-like kinase 1, shows broad-spectrum preclinical antitumor activity in multiple dosing regimens. Mol Cancer Ther. 2012 Mar;11(3):700-9. 2. Inoue M, et al. PLK1 blockade enhances therapeutic effects of radiation by inducing cell cycle arrest at the mitotic phase. Sci Rep. 2015 Oct 27;5:15666.
- 溶解性: DMSO : 16.67 mg/mL (29.68 mM; ultrasonic and warming and heat to 60°C)
- 保存條件: RT
- 配置溶液濃度參考:
1mg 5mg 10mg 1 mM 1.781 ml 8.903 ml 17.806 ml 5 mM 0.356 ml 1.781 ml 3.561 ml 10 mM 0.178 ml 0.89 ml 1.781 ml 50 mM 0.036 ml 0.178 ml 0.356 ml
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輸入產(chǎn)品批號(hào):
本計(jì)算器可幫助您計(jì)算出特定溶液中溶質(zhì)的質(zhì)量、溶液濃度和體積之間的關(guān)系,公式為:
質(zhì)量 (mg) = 濃度 (mM) x 體積 (mL) x 分子摩爾量 (g/mol)