貨號(hào)	規(guī)格	價(jià)格	上海	北京	武漢	南京
S81189-5mg	99%	￥510.00 S81189-5mg ￥510.00 現(xiàn)貨	7 7	-	-	-
S81189-10mg	99%	￥765.00 S81189-10mg ￥765.00 現(xiàn)貨	6 6	-	-	-
S81189-50mg	99%	￥1955.00 S81189-50mg ￥1955.00 現(xiàn)貨	6 6	-	-	-
S81189-100mg	99%	￥3000.00 S81189-100mg ￥3000.00 2-3天	0 貨期：2-3天	-	-	-

貨號(hào)

規(guī)格

價(jià)格

上海

北京

武漢

南京

購(gòu)買數(shù)量

S81189-5mg

99%

￥510.00

S81189-10mg

99%

￥765.00

S81189-50mg

99%

￥1955.00

S81189-100mg

99%

￥3000.00

貨期：2-3天

產(chǎn)品介紹

NMS-1286937 is a potent, selective and orally available PLK1 inhibitor, with an IC50 of 2 nM.

產(chǎn)品描述：

NMS-1286937 is a potent, selective and orally available PLK1 inhibitor, with an IC50 of 2 nM.

靶點(diǎn)：

PLK1:2 nM (IC50);MELK:744 nM (IC50);CK2:826 nM (IC50);FLT:510 nM (IC50);Apoptosis;?PLK

體外研究：

NMS-1286937 is a potent, selective and orally available PLK1 inhibitor, with IC50 of 2 nM. NMS-1286937 also shows inhibitory activities against FLT3, MELK, and CK2, with IC50s of 510, 744, and 826 nM, respectively. NMS-P937 possesses a pure ATP competitive mechanism with a reversible dissociation and no time dependency. NMS-P937 (10 μM) is selective with a marginal activity of 48% and 40% inhibition on PLK2 and PLK3, respectively. NMS-P937 shows antiproliferative activity against a panel of 137 cell lines, with IC50 values of below 100 nM for 60 of 137 cell lines and higher than 1 μM for only 9 of 137 cell lines. NMS-P937 shows cytotoxic activity against AmL-NS8 cells with IC50 of 36 nM.

體內(nèi)研究：

NMS-1286937 (45 mg/kg, i.v.) shows a good tumor growth inhibition with acceptable and reversible body weight loss in CD1 nu/nu mice xenografted with human HCT116 colon adenocarcinoma cells. NMS-1286937 (60 mg/kg, p.o.) also inhibits the growth of tumor on HCT116 xenograft model. NMS-P937 (45 mg/kg, i.v.or 60 mg/kg, p.o) inhibits tumor growth to a comparable degree (TGI, 83% and 79% intravenously and orally, respectively) in HCT116-bearing mice. The combination of NMS-P937 (120 mg/kg given for 4 cycles of 2 consecutive days with 10-day rest) and cytarabine (75 mg/kg for 4 cycles of 5 consecutive days with 7-day rest) in the disseminated leukemia model AmL-PS is well tolerated and clearly showed increased mice survival. NMS-P937 (60 mg/kg bid os per day over 2 days with a 5 day rest) shows good efficacy compared to standard therapies, with a significant increase in median survival time (MST) in the established disease setting.

參考文獻(xiàn)：

1. Beria I, et al. NMS-P937, a 4,5-dihydro-1H-pyrazolo[4,3-h]quinazoline derivative as potent and selective Polo-like kinase 1 inhibitor. Bioorg Med Chem Lett. 2011 May 15;21(10):2969-74.
2. Valsasina B, et al. NMS-P937, an orally available, specific small-molecule polo-like kinase 1 inhibitor with antitumor activity in solid and hematologic malignancies. Mol Cancer Ther. 2012 Apr;11(4):1006-16.
3. Casolaro A, et al. The Polo-Like Kinase 1 (PLK1) inhibitor NMS-P937 is effective in a new model of disseminated primary CD56+ acute monoblastic leukaemia. PLoS One. 2013;8(3):e58424.

溶解性：

soluble in DMSO

保存條件：

-20℃

配置溶液濃度參考：

	1mg	5mg	10mg
1 mM	1.878 ml	9.389 ml	18.779 ml
5 mM	0.376 ml	1.878 ml	3.756 ml
10 mM	0.188 ml	0.939 ml	1.878 ml
50 mM	0.038 ml	0.188 ml	0.376 ml

注意：

部分產(chǎn)品我司僅能提供部分信息，我司不保證所提供信息的權(quán)威性，僅供客戶參考交流研究之用。

參考文獻(xiàn)

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計(jì)算重置

NMS-1286937

1-(2-hydroxyethyl)-8-((5-(4-methylpiperazin-1-yl)-2-(trifluoromethoxy)phenyl)amino)-4,5-dihydro-1H-pyrazolo[4,3-h]quinazoline-3-carboxamide