Home Protein Tyrosine Kinase c-Met inhibitor - Axl inhibitor NPS-1034 For research use only.

NPS-1034

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

NPS-1034 Chemical Structure

NPS-1034 Chemical Structure

CAS No. 1221713-92-3

Purity & Quality Control

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

NPS-1034 Related Products

Signaling Pathway

c-Met Signaling Pathways

c-Met Signaling Pathway

Biological Activity

Description NPS-1034 is a dual Met (c-Met)/Axl inhibitor with IC50 of 48 nM and 10.3 nM, respectively.
Targets
Axl [1]
(Cell-free assay)		 Met [1]
(Cell-free assay)
10.3 nM 48 nM
In vitro
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, NPS-1034 enhances sensitivity to EGFR-TKIs. In HCC78 cells, NPS-1034 inhibits ROS1 activity and cell proliferation. In addition, a combination of gefitinib and NPS-1034 enhances cell death by inducing caspase-3 and PARP-1 cleavage. [1] NPS-1034 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. [2]
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.
Cell Research Cell lines HCC827/GR, HCC-78 and H820 cells
Concentrations ~5 μM
Incubation Time 72 h
Method To perform the MTT assay, cells (0.5 × 104/well) are plated in 96-well sterile plastic plates and allowed to attach overnight. Cells are exposed to varying doses of gefitinib, erlotinib, PHA-665752, and NPS-1034 in medium containing 1% FBS. After 72 hours, 15 μL of MTT solution (5 mg/mL) is added to each well and plates are incubated for 4 hours. Crystalline formazan is solubilized with 100 μL of a 10% (w/v) SDS solution for 24 hours. Absorbance at 595 nm is read spectrophotometrically using a microplate reader.
Experimental Result Images Methods Biomarkers Images PMID
Growth inhibition assay Cell viability 29144989
In Vivo
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 NPS-1034 results in enhanced tumor growth inhibition via the inhibition of tumor proliferation and the induction of apoptosis. [1] In nude mice bearing MKN45 xenograft tumors, NPS-1034 (30 mg/kg, p.o.) decreases tumor growth through the inhibition of angiogenesis and the promotion of apoptosis. [2]
Animal Research Animal Models SCID mice bearing HCC827/GR tumor xenografts
Dosages 10 mg/kg, 5 days a week
Administration p.o.

Chemical Information & Solubility

Molecular Weight 551.54 Formula

C31H23F2N5O3
CAS No. 1221713-92-3 SDF Download NPS-1034 SDF
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
Storage (From the date of receipt)

In vitro
Batch:

DMSO : 100 mg/mL ( (181.31 mM) Moisture-absorbing DMSO reduces solubility. Please use fresh DMSO.)

Ethanol : 4 mg/mL

Water : Insoluble


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In vivo
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Tech Support

Answers to questions you may have can be found in the inhibitor handling instructions. Topics include how to prepare stock solutions, how to store inhibitors, and issues that need special attention for cell-based assays and animal experiments.

Handling Instructions

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