NPS-1034 产品说明书 Chemicals
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产品编号 DC8398
名称 NPS-1034

化学性质

CAS 1221713-92-3
分子式 C31H23F2N5O3
分子量 551.54
存储条件 2 years -20°C Powder, 2 weeks 4°C in DMSO, 6 months -80°C in DMSO

生物活性

Description
In Vivo
In Vitro

化合物的使用

Kinase Assay
Cell Assay
Animal Administration

参考文献


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.
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