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PF-04217903 (PF-4217903) is a novel ATP-competitive small molecule inhibitor of c-Met kinases with the IC50 values from 3.1 nM to 142 nM. PF-04217903 (PF-4217903) demonstrated >1000 fold selectivity for c-Met compared with >150 kinases, making it one of the most selective c-Met inhibitors described to date. PF-04217903 (PF-4217903) inhibited tumor cell proliferation, survival, migration/invasion in MET amplified cell lines in vitro, and demonstrated marked antitumor activity in tumor models harboring either MET gene amplification or a HGF/c-Met autocrine loop at well-tolerated dose levels in vivo.
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Application | mice treatment in vivo and histological evaluation |
| Results | "Systemic administration of PF-04217903 decreased the weight and volume of B16F10 melanomas by 36% and 54%, respectively. Instead, MET knockdown in cancer cells only, led to 58% and 75% inhibition of tumour growth and volume.TAN inhibition by PF-04217903 was comparable in both Met-silenced and scrambled B16F10 melanomas." |
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Application | mice treatment in vivo and histological evaluation |
| Results | Systemic treatment of WT mice carrying B16F10 melanomas (which are dependent on MET14) with three different MET tyrosine-kinase inhibitors (PF-04217903, INCB28060 and JNJ-38877605), strongly reduced TAN recruitment . |
| Cell Experiment | |
|---|---|
| Cell lines | B16F1, Tib6, EL4, and LLC, and endothelial cells, HUVECs and C166 |
| Preparation method | Cell lines, including B16F1, Tib6, EL4, and LLC, and endothelial cells, HUVECs and C166, were seeded at 104 cells in each well of 24-well tissue culture–treated plates. Cells were grown in the standard media as described earlier. Cells were treated with different concentrations (2, 0.2, and 0.02 μmol/L) of sunitinib, PF-04217903, and combination of both compounds for 4 days. Efficacy of the compounds was measured by counting cells in a Coulter counter machine (BD Biosciences). Similar approach was applied to evaluate the role of HGF or VEGF on cell proliferation, using 3 different concentrations (10, 100, and 200 ng/mL) of each ligand. |
| Concentrations | 2, 0.2, and 0.02 μmol/L |
| Incubation time | 4 days |
| Animal Experiment | |
|---|---|
| Animal models | B16F10 tumour-bearing mice |
| Formulation | 0.5% methylcellulose in saline |
| Dosages | 40mg/kg PF-04217903 |
| Administration | oral |
| Molecular Weight | 372.38 |
| Formula | C19H16N8O |
| CAS Number | 956905-27-4 |
| Solubility (25°C) | DMSO 15 mg/mL |
| Storage |
Powder -20°C 3 years ; 4°C 2 years In solvent -80°C 6 months ; -20°C 1 month |
| Best-selling c-Met Products |
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| 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. |
| Foretinib
Foretinib (XL880, GSK1363089) is a multi-targeted inhibitor of c-Met and vascular endothelial growth factor receptor 2 (VEGFR2) with IC50 value of 0.4 nM for c-MET. |
| Crizotinib
Crizotinib (PF-02341066) is a potent, orally bioavailable, ATP-competitive small-molecule inhibitor of c-Met kinase and ALK (anaplastic lymphoma kinase) with IC50 values to be 4 and 25 nM for C-Met and ALK resepectively. |
| Golvatinib
Golvatinib (E7050) is an orally bioavailable dual kinase inhibitor of c-Met and VEGFR-2 tyrosine kinases with potential antineoplastic activity. |
| Capmatinib (INCB28060)
Capmatinib (INCB28060) is a novel inhibitor of c-MET kinase with IC50 of 0.13 nM. |
| Other c-Met Products |
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| 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. |
| SGX523
SGX523 is an exquisitely selective, ATP-competitive inhibitor of the MET receptor tyrosine kinase with antitumor activity in vivo. |
| JNJ-38877605
JNJ-38877605 is a small-molecule, ATP-competitive inhibitor of the catalytic activity of c-Met with an IC50 of 4 nM. |
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