貨號	規格	價格	上海	北京	武漢	南京	購買數量
S82312-5mg	≥99%	￥1580.00 S82312-5mg ￥1580.00 2-3天	0 貨期：2-3天	-	-	-
S82312-10mg	≥99%	￥2500.00 S82312-10mg ￥2500.00 2-3天	0 貨期：2-3天	-	-	-

產品介紹

NMS-P715 is a selective, ATP-competitive inhibitor of MPS1, with an IC50 of 182 nM.

產品描述：

NMS-P715 is a selective, ATP-competitive inhibitor of MPS1, with an IC50 of 182 nM.

靶點：

Mps1:182 nM (IC50);CK2:5.7 μM (IC50);MELK:6.01 μM (IC50);NEK6:6.02 μM (IC50);CaseinKinase;?Kinesin;?MELK;?MAPK

體外研究：

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

體內研究：

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

參考文獻：

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.

溶解性：

soluble in DMSO

保存條件：

-20℃

配置溶液濃度參考：

	1mg	5mg	10mg
1 mM	1.478 ml	7.388 ml	14.777 ml
5 mM	0.296 ml	1.478 ml	2.955 ml
10 mM	0.148 ml	0.739 ml	1.478 ml
50 mM	0.03 ml	0.148 ml	0.296 ml

注意：

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

參考文獻

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