NPS-1034是一种双Met (c-Met)/Axl抑制剂，IC50分别为48 nM和10 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
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NPS-1034
Dangerous GoodsCAS number：1221713-92-3 molecular formula：C31H23F2N5O3
overview
compound introduction
Specs
| Chinese alias | 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 | ||
| English alias | - | ||
| CAS number | 1221713-92-3 | molecular formula | C31H23F2N5O3 |
| molecular weight | 551.54 g/mol | Exact mass | 10mM in DMSO |
| PSA | 90.600 Ų | logp | 4.795 |
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Safety information
pictogram：
GHS07
Signal word：
Warning
Hazard Statement：
H302: 吞食有害
Statement of Preventive Measures：
P305+P351+P338: 如进入眼睛：用水小心冲洗几分钟。如戴隐形眼镜并可方便地取出，取出隐形眼镜。继续冲洗。 P280: 戴防护手套/穿防护服/戴防护眼罩/戴防护面具。
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