| References: |
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. 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. 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. 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. 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. |
