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merck millipore,默克密理博,475949,MPS1 Inhibitor, NMS-P715 - Calbiochem
产品名称：MPS1 Inhibitor, NMS-P715 - Calbiochem
产品型号：475949
The MPS1 Inhibitor, NMS-P715 controls the biological activity of MPS1. This small molecule/inhibitor is primarily used for Phosphorylation & Dephosphorylation applications.
merck millipore,默克密理博,475949,MPS1 Inhibitor, NMS-P715 - Calbiochem
- 产品介绍
重要规格表
经验配方 C₃₅H₃₉F₃N₈O₃ 描述 概述 An orally bioavailable, ATP-competitive, pyrazolo-quinazoline, MPS1 inhibitor (IC50 = 182 nM, Ki = 0.99 nM) that is shown to act in a reversible and time-dependent manner. It demonstrates selectivity for MPS1 against a panel of 60 kinases, displaying activity against only three kinases, CK2, MELK, and NEK6 (< 10 µM), but not against other mitotic kinases including PLK1, CDK1, Aurora A, Aurora B, or the SAC kinase BUB1, in an in vitro kinase assay. It promotes massive SAC (spindle assembly checkpoint) override (EC50 = 65 nM) in nocodazole-arrested U20S cells and elicits a reduction in the G1 and G2/M phase of the cell cycle in A2780 ovarian cancer cells, similar to RNAi-mediated MPS1 silencing. In addition, it is shown to inactivate SAC, delocalize kinetochore components, and inhibit the proliferation of select cancer cell lines (IC50 ~ 1 µM), without marked activity among a panel of 127 normal cell lines. Also, it inhibits A2780 tumor xenograft growth in mice (90 mg/kg/day, o.s., in vivo) by 53% without marked body weight loss. Also available as a 5 mM solution in DMSO (Cat. No. 506313). 产品目录编号 475949 品牌系列 Calbiochem®
同义词 (N-(2,6-diethylphenyl)-1-methyl-8-({4-[(1-methylpiperidin-4-yl)carbamoyl]-2-(trifluoromethoxy)phenyl}amino)-4,5-dihydro-1H-pyrazolo[4,3-h]quinazoline-3-carboxamide) 参考 参考 Caldarelli, M., et al. 2011. Bioorg. Med. Chem. Lett. 21, 4507.
Colombo, R., et al. 2011. Cancer Res. 70, 10255.产品信息 形式 White powder Hill配方 C₃₅H₃₉F₃N₈O₃ 化学配方 C₃₅H₃₉F₃N₈O₃ Molar Mass 676.31 结构配方图像 生物信息 纯度 ≥98% by HPLC 储存和货运信息 货运代码 Ambient Temperature Only
毒性 Standard Handling
储存 +2°C to +8°C
避光 Protect from light
无需冷冻 No
特殊指南 Following reconstitution, aliquot and freeze (-20°C). Stock solutions are stable for up to 3 months at -20°C. 包装信息 惰性气体下包装 Packaged under inert gas
上一件merck millipore产品：merck millipore,默克密理博,TR-1001,GPT Selection Reagent, 500X Mycophenolic Acid; 100X Aminopterin
下一件merck millipore产品：merck millipore,默克密理博,252718,n-Decyl-β-D-maltopyranoside, ULTROL Grade - CAS 82494-09-5 - Calbiochem
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