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.
Protect the integrity of proteins from multiple proteases and phosphatases for different applications.
NPS-1034 is a MET inhibitor with IC50 of 4 nmol/L .
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 .
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 .
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 .
. 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|
|Solubility||Soluble in DMSO|