2016年1月5日星期二

NPS-1034|cas 1221713-92-3|DC Chemicals

NPS-1034|cas 1221713-92-3|DC Chemicals

NPS-1034 is a dual Met/Axl inhibitor with IC50 of 48 nM and 10.3 nM, respectively.

Product Name: NPS-1034 |Catalog Number: DC8398 |CAS 1221713-92-3 |Other names:  |Chemical Name: N-(3-fluoro-4-(3-phenyl-1H-pyrrolo[2,3-b]pyridin-4-yloxy)phenyl)-2-(4-fluorophenyl)-1,5-dimethyl-3-oxo-2,3-dihydro-1H-pyrazole-4-carboxamide |Molecule Formular: C31H23F2N5O3 |MW: 551.54

In HCC827/GR cells, NPS-1034 does not show significant antiproliferative effects, while overcomes gefitinib resistance by inhibiting the phosphorylation of MET, Akt, and Erk. In H820 cells, NPS-1034 enhances sensitivity to EGFR-TKIs. In HCC78 cells, NPS-1034 inhibits ROS1 activity and cell proliferation. In addition, a combination of gefitinib and NPS-1034 enhances cell death by inducing caspase-3 and PARP-1 cleavage. [1] NPS-1034 inhibits the viability of the MKN45 and SNU638 cell lines, which highly express the MET gene and p-MET, with IC50 of 112.7 and 190.3 nmol, respectively. [2]In SCID mice bearing HCC827/GR tumor xenografts, NPS-1034 (10 mg/kg, p.o.) decreases tumor growth, and the combination of gefitinib and NPS-1034 results in enhanced tumor growth inhibition via the inhibition of tumor proliferation and the induction of apoptosis. [1] In nude mice bearing MKN45 xenograft tumors, NPS-1034 (30 mg/kg, p.o.) decreases tumor growth through the inhibition of angiogenesis and the promotion of apoptosis. [2] For the detailed information of  NPS-1034, the solubility of  NPS-1034 in water, the solubility of  NPS-1034 in DMSO, the solubility of  NPS-1034 in PBS buffer, the animal experiment (test) of   NPS-1034, the cell expriment (test) of  NPS-1034, the in vivo, in vitro and clinical trial test of  NPS-1034, the EC50, IC50,and affinity,of  NPS-1034, For the detailed information of  NPS-1034, the solubility of  NPS-1034 in water, the solubility of  NPS-1034 in DMSO, the solubility of  NPS-1034 in PBS buffer, the animal experiment (test) of   NPS-1034, the cell expriment (test) of  NPS-1034, the in vivo, in vitro and clinical trial test of  NPS-1034, the EC50, IC50,and affinity,of  NPS-1034, Please contact DC Chemicals.

For research and scientific purpose only, not for human use.

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