NMS-P715|1202055-32-0|-陌孚医药/Medlife

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NMS-P715

目录号: PL07534 纯度: ≥99%

CAS No. :1202055-32-0

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中文名称	NMS-P715
中文别名	NMS-P715
英文名称	NMS-P715
英文别名	NMS-P715;NMS P715;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;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;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;N-(2,6-diethylphenyl)-1-methyl-8-[4-[(1-methylpiperidin-4-yl)carbamoyl]-2-(trifluoromethoxy)anilino]-4,5-dihydropyrazolo[4,3-h]quinazoline
Cas No.	1202055-32-0
分子式	C₃₅H₃₉F₃N₈O₃
分子量	676.73
包装储存	Powder -20°C 3 years；4°C 2 years

产品详情	NMS-P715 是一种选择性的，ATP 竞争性的 MPS1 抑制剂，IC₅₀ 值为 182 nM。
生物活性	NMS-P715 is a selective, ATP-competitive inhibitor of MPS1, with an IC 50 of 182 nM.
性状	Solid
IC50 & Target[1][2]	Mps1 182 nM (IC50) CK2 5.7 μM (IC50
体外研究(In Vitro)	NMS-P715 is a selective inhibitor of MPS1, with an IC50 of 182 nM. NMS-P715 is highly specific for MPS1, with no other kinases inhibited below an IC50 value of 5 μM and only 3 kinases inhibited below 10 μM (CK2, MELK, and NEK6). NMS-P715 promotes massive spindle assembly checkpoint (SAC) override with an EC50 of 65 nM. NMS-P715 (1 μM) causes mitotic acceleration in U2OS cells overexpressing YFP-α-tubulin, induces aneuploidy and inhibits the proliferation of HCT116 cells. NMS-P715 (0.5, 1 μM) affects mitotic checkpoint complex (MCC) stability and cdc20 ubiquitylation. NMS-P715 (1 μM) exhibits bypass of the spindle assembly checkpoint and apoptosis in pancreatic ductal adenocarcinoma (PDAC) cell lines. NMS-P715 (0-25 μM) also selectively inhibits growth of PDAC cells. has not independently
体内研究(In Vivo)	NMS-P715 (10 mg/kg) exhibits an oral bioavailability of 37% and good pharmacokinetic properties in nude mice bearing subcutaneous implanted human tumor cell xenografts. NMS-P715 (90 mg/kg, p.o.) is well tolerated and cuases no signs of body weight loss or other overt toxicities in an A2780 ovary carcinoma xenograft model. NMS-P715 (100 mg/kg, p.o.) inhibits the tumor growth by appr 43% in the A375 melanoma xenograft model. has not independently confirmed the accuracy of these methods. They are for reference only.
运输条件	Room temperature in continental US; may vary elsewhere.
储存方式	Powder -20°C 3 years；4°C 2 years
参考文献	[1]. Colombo R, et al. Targeting the mitotic checkpoint for cancer therapy with NMS-P715, an inhibitor of MPS1 kinase. Cancer Res. 2010 Dec 15;70(24):10255-64. [2]. Slee RB, et al. Selective inhibition of pancreatic ductal adenocarcinoma cell growth by the mitotic MPS1 kinase inhibitor NMS-P715. Mol Cancer Ther. 2014 Feb;13(2):307-315.

溶解度数据	In Vitro: DMSO : 2 mg/mL (2.96 mM; Need ultrasonic)配制储备液

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1：一般建议：溶解度为Medlife测试数据，可能与文献描述存在差异。这是由于生产工艺和批次不同产生的正常现象。为了使其更好的溶解，请用37℃加热试管并在超声波水浴中震动片刻。不同批次产品溶解度各有差异，仅做参考，具体以实验方案为准。

2：储存条件：粉末-20°C一般情况可以保存3年，溶于溶剂-80°C一般情况可以保存1年。不同产品及不同批次产品可能存在差异，请细致阅读产品信息，并辅助参考相关文献描述。

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