NPS-1034

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Chemical Structure| 1221713-92-3 同义名 : -
CAS号 : 1221713-92-3
货号 : A518169
分子式 : C31H23F2N5O3
纯度 : 99%+
分子量 : 551.543
MDL号 : MFCD29905447
存储条件：

Pure form Sealed in dry,Store in freezer, under -20°C

In solvent -20°C:3-6个月-80°C:12个月
溶解度 :

DMSO: 35 mg/mL(63.46 mM)，配合低频超声助溶，注意：DMSO长时间开封后，会吸水并导致溶解能力下降，请避免使用长期开封的DMSO
动物实验配方：
生物活性
描述 NPS-1034 serves as a dual antagonist for AXL and MET, exhibiting IC50 values of 10.3 nM for AXL and 48 nM for MET. In HCC827/ER cells, where AXL's expression and activity are notably heightened, treatment with NPS-1034 successfully curtails its tyrosine phosphorylation. NPS-1034 reduces the viability of MKN45 and SNU638 cell lines, which have high expression levels of the MET gene and phosphorylated MET, with IC50 values of 112.7 nM and 190.3 nM, respectively. Conversely, it inhibits the viability of AGS, KATOIII, NCI-N87, MKN1, MKN28, and MKN74 cell lines with IC50 values ranging from 1 μM to over 10 μM. Treatment with NPS-1034 significantly lowers MET phosphorylation in MKN45 cells, but not in MKN28 cells. It also inhibits HGF-induced MET autophosphorylation in AGS and MKN1 cell lines with IC50 values of less than 10 nM and less than 50 nM, respectively, with 50 nM of NPS-1034 completely blocking HGF-induced MET phosphorylation[1].
实验方案
1mg 5mg 10mg

1 mM

5 mM

10 mM

1.81mL

0.36mL

0.18mL

9.07mL

1.81mL

0.91mL

18.13mL

3.63mL

1.81mL
参考文献

[1]Rho JK, et al. MET and AXL inhibitor NPS-1034 exerts efficacy against lung cancer cells resistant to EGFR kinase inhibitors because of MET or AXL activation. Cancer Res. 2014 Jan 1;74(1):253-62.

[2]Shin JS, et al. NPS-1034, a novel MET inhibitor, inhibits the activated MET receptor and its constitutively active mutants. Invest New Drugs. 2014 Jun;32(3):389-99.