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PHA-665752 is a small-molecule inhibitor of c-Met, inhibits tumorigenicity and angiogenesis in mouse lung cancer xenografts. c-Met is a tyrosine kinase receptor for hepatocyte growth factor/scatter factor (HGF/SF). PHA665752 inhibited specific phosphorylation of TPR-MET as well as phosphorylation of downstream targets of the mammalian target of rapamycin pathway. Short-term treatment with PHA-665752 decreased the numbers of premalignant lung lesions and induced apoptosis in tumor cells and vascular endothelial cells within lesions. In cell culture, PHA-665752 induced apoptosis of a lung adenocarcinoma cell line derived from Kras(LA1) mice (LKR-13) and a murine lung endothelial cell line (MEC). PHA665752 was shown to inhibit cMet/HGF/SF signaling in vitro, suggesting c-Met inhibitors may have efficacy for blocking local progression and/or metastatic spread of c-Met-positive NBL in vivo.
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Source | Biochem Biophys Res Commun (2014). Figure 2.PHA-665752 |
| Method | MTT assay | |
| Cell Lines | CNE-1 and HONE-1 cells | |
| Concentrations | 2 μM | |
| Incubation Time | 72 h | |
| Results | Further experiments showed that PHA-665752 inhibited cell proliferation in a dose-dependent manner in the CNE-1 and HONE-1 cells |
| Cell Experiment | |
|---|---|
| Cell lines | S114, GTL-16, NCI-H441, or BxPC-3 cells |
| Preparation method | Cell Proliferation Assays. S114, GTL-16, NCI-H441, or BxPC-3 cells were seeded in 96-well plates at 9000 cells/well in medium with 10% FBS. After incubation for 48 h in low serum (0.5% FBS, S114; 0.1% FBS, GTL-16, NCI-H441, and BxPC-3), cells were treated with different concentrations of PHA-665752 for 18 h at 37°C. HGF (50 ng/ml) was added for 18 h before BrdUrd for studies involving GTL-16, H441, and BxPC-3. After incubation with BrdUrd labeling reagent for 1 h, cells were fixed and BrdUrd incorporation into newly synthesized DNA was assessed using anti-BrdUrd peroxidase-conjugated antibody followed by colorimetric determination at 630 nm. |
| Concentrations | 0~1.25µM |
| Incubation time | 18h |
| Animal Experiment | |
|---|---|
| Animal models | athymic mice bearing S114 or GTL-16 tumor xenografts |
| Formulation | L-lactate (pH 4.8) and 10% polyethylene glycol |
| Dosages | 7.5, 15, 30 mg/kg/day |
| Administration | i.v. bolus via tail vein injection |
| Molecular Weight | 641.61 |
| Formula | C32H34Cl2N4O4S |
| CAS Number | 477575-56-7 |
| Solubility (25°C) | DMSO 60 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 |
|---|
| AMG-208
AMG-208 is a potent small molecular inhibitor c-Met with an IC50 of 9.3 nM. AMG-208 is also a CYP3A4 inhibitor with an IC50 of 32 μM. AMG-208 has anti-cancer activity. |
| BMS-777607
BMS-777607 is a selective and potent small-molecule met kinase inhibitor for c-Met, Axl, Ron and Tyro3 with IC50s of 3.9 nM, 1.1 nM, 1.8 nM and 4.3 nM, respectively. |
| BMS 794833
BMS-794833 is a potent ATP competitive Met/VEGFR-2 kinase inhibitor. |
| AMG-458
AMG-458 is a potent, selective and orally bioavailable c-Met inhibitor, with Ki values of 1.2 nM and 2.0 nM for human and mouse c-Met, respectively. |
| XL-184
Cabozantinib (XL184, BMS-907351) is a small molecule inhibits multiple receptor tyrosine kinases, specifically MET and VEGFR2 with IC50 values of 0.035 and 1.8 nM for VEGFR2 and Met respectively. |
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