NPS-1034
规格
| Cas Number | 1221713-92-3 |
| 规格或纯度 | ≥97% |
| 纯度 | ≥97% |
| 包装 | 100mg 或 50mg 或 10mg 或 5mg 或 25mg |
产品信息
| 别名 | 2-(4-氟苯基)-N-[3-氟-4-[(3-苯基-1H-吡咯并[2,3-B]吡啶-4-基)氧基]苯基]-2,3-二氢-1,5-二甲基-3-氧代-1H-吡唑-4-甲酰胺 |
| 品牌 | 阿拉丁 |
| 溶解性 | Solubility (25°C) In vitro DMSO: 100 mg/mL warmed with 50ºC Water: bath (181.31 mM); Ethanol: 4 mg/mL (7.25 mM); Water: Insoluble; |
| 简短描述 | Axl 抑制剂 |
| 英文简短描述 | Axl Inhibitors |
| 过滤标签 | c-Met/HGFR,TAM Receptor,Protein Tyrosine Kinase/RTK |
| 储存温度 | -20°C储存 |
| 运输条件 | 超低温冰袋运输 |
| 生化和生理学机理 | NPS-1034 是一种 Met（c-Met）/Axl 双重抑制剂，其 IC50 分别为 48 nM 和 10.3 nM。 |
| 描述 |
NPS-1034是一种双Met (c-Met)/Axl抑制剂，IC50分别为48 nM和10 |
| 英文描述 |
Information NPS-1034 NPS-1034 is a dual Met (c-Met)/Axl inhibitor with IC50 of 48 nM and 10.3 nM, respectively. Targets Axl (Cell-free assay); Met (Cell-free assay) 10.3 nM; 48 nM In vitro 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 vivo 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. Cell Research(from reference) Cell lines：HCC827/GR, HCC-78 and H820 cells Concentrations：~5 μM Incubation Time：72 h |