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NPS-1034

现货
Catalog No.
B6006
MET抑制剂
组合的产品项目
规格价格库存 数量
5mg
¥ 1,050.00
Ship with 10-15 days
25mg
¥ 3,350.00
Ship with 10-15 days
100mg
¥ 6,850.00
Ship with 10-15 days

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Background

NPS-1034 is a MET inhibitor with IC50 of 4 nmol/L [1].

The hepatocyte growth factor receptor tyrosine kinase MET is required for various morphogenetic events and controls the malignant progression of many human tumors. In various advanced human cancer, gene amplification can deregulate MET [1].

In MKN45 and SNU638 cell lines highly expressing the MET gene and p-MET (phosphorylated MET), IC50 values of NPS-1034 to inhibit cell viability were 112.7 and 190.3 nmol, respectively. In AGS, KATOIII, NCI-N87, MKN1, MKN28, and MKN74 cells, the IC50 values of NPS-1034 to inhibit cell viability ranged from 1 μmol to more than 10 μmol. In MKN45 cells, treatment with NPS-1034 dramatically decreased MET phosphorylation (activation). But in MKN28 cells, MET phosphorylation was not dramatically decreased. This meant that the anti-proliferative effect of NPS-1034 was resulted from its inhibition of p-MET [1].

In nude mice bearing MKN45 tumors, after the diameter of MKN45 tumors had reached about 180 mm3, NPS-1034 at a dose of 30 mg/kg or PBS as vehicle was orally administered once daily for 25 days. It was found that NPS-1034 inhibited the proliferation of tumors highly expressing p-MET. Without drug treatment, neovascularization appeared in tumors in nude mice when the tumor volume was >150 mm3. NPS-1034 treatment clearly decreased the vascularization of the tumors in nude mice [1].

Reference:
[1].  Shin JS, Hong SW, Moon JH, et al. NPS-1034, a novel MET inhibitor, inhibits the activated MET receptor and its constitutively active mutants. Investigational new drugs, 2014, 32(3): 389-399.

Chemical Properties

Physical AppearanceA crystalline solid
StorageStore at -20°C
M.Wt551.54
Cas No.1221713-92-3
FormulaC31H23F2N5O3
SolubilitySoluble in DMSO
Chemical NameN-(3-fluoro-4-((3-phenyl-1H-pyrrolo[2,3-b]pyridin-4-yl)oxy)phenyl)-2-(4-fluorophenyl)-1,5-dimethyl-3-oxo-2,3-dihydro-1H-pyrazole-4-carboxamide
SDFDownload SDF
Canonical SMILESFC1=CC(NC(C2=C(C)N(C)N(C3=CC=C(F)C=C3)C2=O)=O)=CC=C1OC4=CC=NC5=C4C(C6=CC=CC=C6)=CN5
运输条件试用装:蓝冰运输。 其他可选规格:常温运输或根据您的要求用蓝冰运输。
一般建议为了使其更好的溶解,请用37℃加热试管并在超声波水浴中震动片刻。不同厂家不同批次产品溶解度各有差异,仅做参考。若实验所需浓度过大至产品溶解极限,请添加助溶剂助溶或自行调整浓度。

质量控制

质量控制和MSDS

批次:

化学结构

NPS-1034