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Cat. No. M9005
NPS-1034 Structure
Size Price Availability Quantity
5mg USD 80  USD80 In stock
10mg USD 120  USD120 In stock
25mg USD 250  USD250 In stock
50mg USD 400  USD400 In stock
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Quality Control & Documentation
Biological Activity

NPS-1034 is a dual inhibitor of Axl and MET with IC50 values of 10.3 and 48 nM, respectively. NPS-1034 inhibits the viability of the MKN45 and SNU638 cell lines, which highly express the MET gene and p-MET (phosphorylated MET), with IC50 values of 112.7 and 190.3 nmol, respectively. NPS-1034 also inhibits hepatocyte growth factor (HGF)-stimulated MET autophosphorylation (Y1234/1235) in the AGS and MKN1 cell lines with IC50 values of <10 and <50 nmol, respectively.

In vivo, NPS-1034 (10 mg/kg, p.o.) decreases tumor growth in SCID mice bearing HCC827/GR tumor xenografts. 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.

Protocol (for reference only)
Cell Experiment
Cell lines HCC827/GR, HCC-78 and H820 cells
Preparation 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.
Concentrations ~5 μM
Incubation time 72 h
Animal Experiment
Animal models SCID mice bearing HCC827/GR tumor xenografts
Formulation PBS
Dosages 10 mg/kg, 5 days a week
Administration p.o.
Chemical Information
Molecular Weight 551.54
Formula C31H23F2N5O3
CAS Number 1221713-92-3
Solubility (25°C) DMSO: ≥ 40 mg/mL warmed
Storage Powder          -20°C   3 years ;  4°C   2 years
In solvent       -80°C   6 months ;  -20°C   1 month
Conversion of different model animals based on BSA (PMID: 27057123)
Species Mouse Rat Rabbit Guinea pig Hamster Dog
Weight (kg) 0.02 0.15 1.8 0.4 0.08 10
Body Surface Area (m2) 0.007 0.025 0.15 0.05 0.02 0.5
Km factor 3 6 12 8 5 20
Animal A (mg/kg) = Animal B (mg/kg) multiplied by  Animal B Km
Animal A Km

For example, to modify the dose of Compound A used for a mouse (20 mg/kg) to a dose based on the BSA for a rat, multiply 20 mg/kg by the Km factor for a mouse and then divide by the Km factor for a rat. This calculation results in a rat equivalent dose for Compound A of 10 mg/kg.


[1] Shin JS, et al. Invest New Drugs. NPS-1034, a novel MET inhibitor, inhibits the activated MET receptor and its constitutively active mutants.

[2] Rho JK, et al. Cancer Res. MET and AXL inhibitor NPS-1034 exerts efficacy against lung cancer cells resistant to EGFR kinase inhibitors because of MET or AXL activation.

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Keywords: NPS-1034 supplier, c-Met, inhibitors, activators

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