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NPS-1034

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
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
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.
Conversion of different model animals based on BSA (Value based on data from FDA Draft Guidelines)
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.

Chemical Information
Molecular Weight 551.54
Formula C31H23F2N5O3
CAS Number 1221713-92-3
Purity 99.80%
Solubility DMSO: ≥ 40 mg/mL warmed
Storage at -20°C
References

[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

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