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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.
| 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. |
| Molecular Weight | 551.54 |
| Formula | C31H23F2N5O3 |
| CAS Number | 1221713-92-3 |
| Solubility (25°C) | DMSO 33 mg/mL |
| Storage |
Powder -20°C 3 years ; 4°C 2 years In solvent -80°C 6 months ; -20°C 1 month |
| Related c-Met Products |
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Zurletrectinib (ICP-723) is a potent tyrosine kinase inhibitor. Zurletrectinib serves as an antineoplastic agent. Zurletrectinib can used for research of TRK-mediated related diseases. |
| ABN401
ABN401 is a highly potent and selective ATP-competitive c-MET inhibitor with an IC50 value of 10 nM. |
| (Z)-Semaxanib
(Z)-Semaxanib is a potent tyrosine kinase inhibitor. |
| MET kinase-IN-2
MET kinase-IN-2 is a potent, selective, orally bioavailable MET kinase inhibitor with an IC50 of 7.4 nM. |
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BMS-817378 is a potent and selective inhibitor of MET with IC50 of 1.7 nM. |
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