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NPS-1034

    
≥97%

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.

源葉(MedMol)
S81243 一鍵復(fù)制產(chǎn)品信息
1221713-92-3
C31H23F2N5O3
551.543
NPS1034; NPS-1034; NPS 1034.
貨號 規(guī)格 價格 上海 北京 武漢 南京 購買數(shù)量
S81243-5mg ≥97% ￥340.00 貨期：3-5天 - - -
S81243-10mg ≥97% ￥407.00 10 - - -
S81243-25mg ≥97% ￥600.00 貨期：3-5天 - - -
S81243-50mg ≥97% ￥726.00 8 - - -
S81243-100mg ≥97% ￥1070.00 貨期：3-5天 - - -
產(chǎn)品介紹 參考文獻(xiàn) 質(zhì)檢證書(COA) 摩爾濃度計(jì)算器 相關(guān)產(chǎn)品

產(chǎn)品介紹

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

產(chǎn)品描述： NPS-1034 is a dual inhibitor of AXL and MET with IC50s of 10.3 and 48 nM, respectively.
靶點(diǎn)： 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(nèi)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(xiàn)： 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
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