貨號	規格	價格	上海	北京	武漢	南京
S81243-5mg	≥97%	￥340.00 S81243-5mg ￥340.00 3-5天	0 貨期：3-5天	-	-	-
S81243-10mg	≥97%	￥407.00 S81243-10mg ￥407.00 現貨	10 10	-	-	-
S81243-25mg	≥97%	￥600.00 S81243-25mg ￥600.00 3-5天	0 貨期：3-5天	-	-	-
S81243-50mg	≥97%	￥726.00 S81243-50mg ￥726.00 現貨	8 8	-	-	-
S81243-100mg	≥97%	￥1070.00 S81243-100mg ￥1070.00 3-5天	0 貨期：3-5天	-	-	-

產品介紹

NPS-1034 is a dual inhibitor of AXL and MET with IC50s of 10.3 and 48 nM, respectively.

產品描述：

NPS-1034 is a dual inhibitor of AXL and MET with IC50s of 10.3 and 48 nM, respectively.

靶點：

IC50: 10.3 nM (AXL), 48 nM (MET);Apoptosis;?c-Met/HGFR;?TAMReceptor

體外研究：

NPS-1034 is a dual inhibitor of AXL and MET with IC50s of 10.3 and 48 nM, respectively.The expression and activity of AXL is significantly increased in HCC827/ER cells, and NPS-1034 treatment effectively inhibits its tyrosine phosphorylation. NPS-1034 inhibits the viability of the MKN45 and SNU638 cell lines, which highly express the MET gene and p-MET (phosphorylated MET), with IC50 values of 112.7 and 190.3 nmol, respectively. In contrast, NPS-1034 inhibits AGS, KATOIII, NCI-N87, MKN1, MKN28, and MKN74 cell viability with IC50 values ranging from 1 μmol to more than 10 μmol. MET phosphorylation is dramatically decreased after treatment with NPS-1034 in the MKN45 cells, but not in the MKN28 cells. NPS-1034 inhibits hepatocyte growth factor (HGF)-stimulated MET autophosphorylation (Y1234/1235) in the AGS and MKN1 cell lines with IC50 values of <10 and <50 nmol, respectively. HGF-induced MET phosphorylation is completely inhibited by 50 nmol NPS-1034.

體內研究：

NPS-1034 inhibits tumor proliferation, which highly expresses p-MET. NPS-1034 treatment induces a clear decrease in the vascularization of the tumors. The expression of alpha-smooth muscle actin (α-SMA) is decreased in the tumor sections of mice treated with NPS-1034. NPS-1034-treated mice show virtually no weight loss, indicating that NPS-1034 is generally well tolerated.

參考文獻：

1. Rho JK, et al. MET and AXL inhibitor NPS-1034 exerts efficacy against lung cancer cells resistant to EGFR kinase inhibitors because of MET or AXL activation. Cancer Res. 2014 Jan 1;74(1):253-62.
2. Shin JS, et al. NPS-1034, a novel MET inhibitor, inhibits the activated MET receptor and its constitutively active mutants. Invest New Drugs. 2014 Jun;32(3):389-99.

溶解性：

soluble in DMSO

保存條件：

-20°C

配置溶液濃度參考：

	1mg	5mg	10mg
1 mM	1.813 ml	9.065 ml	18.131 ml
5 mM	0.363 ml	1.813 ml	3.626 ml
10 mM	0.181 ml	0.907 ml	1.813 ml
50 mM	0.036 ml	0.181 ml	0.363 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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NPS-1034

N-(3-fluoro-4-((3-phenyl-1H-pyrrolo[2,3-b]pyridin-4-yl)oxy)phenyl)-2-(4-fluorophenyl)-1,5-dimethyl-3-oxo-2,3-dihydro-1H-pyrazole-4-carboxamide.