NPS-1034
mRNA synthesis
In vitro transcription of capped mRNA with modified nucleotides and Poly(A) tail
Tyramide Signal Amplification (TSA)
TSA (Tyramide Signal Amplification), used for signal amplification of ISH, IHC and IC etc.
Phos Binding Reagent Acrylamide
Separation of phosphorylated and non-phosphorylated proteins without phospho-specific antibody
Cell Counting Kit-8 (CCK-8)
A convenient and sensitive way for cell proliferation assay and cytotoxicity assay
SYBR Safe DNA Gel Stain
Safe and sensitive stain for visualization of DNA or RNA in agarose or acrylamide gels.
Inhibitor Cocktails
Protect the integrity of proteins from multiple proteases and phosphatases for different applications.
NPS-1034是MET的抑制剂,IC50为4 nmol/L[1]。
肝细胞生长因子受体酪氨酸激酶MET对于各种形态发生至关重要,并控制许多人类肿瘤的恶性进展。在各种晚期人类癌症中,基因扩增可以下调MET [1]。
在高表达MET基因和磷酸化MET(p-MET)的MKN45和SNU638细胞系中,NPS-1034抑制细胞存活率,IC50值分别为112.7和190.3 nmol。在AGS、KATOIII、NCI-N87、MKN1、MKN28和MKN74细胞中,NPS-1034抑制细胞活力,IC50值从1 μmol到10 μmol。在MKN45细胞中,NPS-1034显著降低了MET的磷酸化(激活)。但在MKN28细胞中,MET磷酸化并没有显著下降。这意味着,NPS-1034的抗增殖效应是由于其抑制MET磷酸化 [1]。
在MKN45肿瘤裸鼠中,当MKN45肿瘤直径达到约180 mm3时,口服给药剂量为30 mg/kg的NPS-1034或PBS,每日给予一次,持续25天。结果发现,NPS-1034抑制高表达P-MET的肿瘤增殖。未经药物治疗,当肿瘤体积为150 mm3时,裸鼠中肿瘤出现新生血管。NPS-1034明显减少裸鼠中肿瘤的血管形成 [1]。
参考文献:
[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.
Physical Appearance | A crystalline solid |
Storage | Store at -20°C |
M.Wt | 551.54 |
Cas No. | 1221713-92-3 |
Formula | C31H23F2N5O3 |
Solubility | Soluble in DMSO |
Chemical Name | N-(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 |
SDF | Download SDF |
Canonical SMILES | FC1=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 | 蓝冰运输或根据您的需求运输。 |
一般建议 | 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。溶液形式一般不宜长期储存,请尽快用完。 |