Home Protein Tyrosine Kinase c-Met inhibitor NPS-1034

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NPS-1034 c-Met inhibitor

Cat.No.S7669

NPS-1034 is a dual Met (c-Met)/Axl inhibitor with IC50 of 48 nM and 10.3 nM, respectively.
NPS-1034 c-Met inhibitor Chemical Structure

Chemical Structure

Molecular Weight: 551.54

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Quality Control

Batch: S766901 DMSO]100 mg/mL]false]Ethanol]4 mg/mL]false]Water]Insoluble]false Purity: 99.72%
99.72

Solubility

In vitro
Batch:

DMSO : 100 mg/mL (181.31 mM)
(Moisture-contaminated DMSO may reduce solubility. Use fresh, anhydrous DMSO.)

Ethanol : 4 mg/mL

Water : Insoluble

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In vivo
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Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid concentration mg/mL, Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug. )

Method for preparing in vivo formulation: Take μL DMSO master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O, mix and clarify.

Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.

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Chemical Information, Storage & Stability

Molecular Weight 551.54 Formula

C31H23F2N5O3

 Storage (From the date of receipt)
CAS No. 1221713-92-3 Download SDF Storage of Stock Solutions

Synonyms N/A Smiles CC1=C(C(=O)N(N1C)C2=CC=C(C=C2)F)C(=O)NC3=CC(=C(C=C3)OC4=C5C(=CNC5=NC=C4)C6=CC=CC=C6)F

Mechanism of Action

Targets/IC50/Ki
Axl
(Cell-free assay)
10.3 nM
Met
(Cell-free assay)
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, this compound enhances sensitivity to EGFR-TKIs. In HCC78 cells, it inhibits ROS1 activity and cell proliferation. In addition, a combination of gefitinib and this chemical enhances cell death by inducing caspase-3 and PARP-1 cleavage. It 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.
Kinase Assay
Kinase inhibition profile
The in vitro NPS-1034 profile of inhibition of RTKs is analyzed using RTK assay kits according to the manufacturer's protocols.
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 this compound results in enhanced tumor growth inhibition via the inhibition of tumor proliferation and the induction of apoptosis. In nude mice bearing MKN45 xenograft tumors, this chemical (30 mg/kg, p.o.) decreases tumor growth through the inhibition of angiogenesis and the promotion of apoptosis.
References

Applications

Methods Biomarkers Images PMID
Growth inhibition assay Cell viability
S7669-viability1
29144989

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