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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.
Pharmacol Res. 2023 Jan 7;188:106640.
Blocking the HGF-MET Pathway Induces Resolution of Neutrophilic Inflammation by Promoting Neutrophil Apoptosis and Efferocytosis
PF-04217903 purchased from AbMole
Elife. 2019 Sep 19;8. pii: e47460.
A distinct cardiopharyngeal mesoderm genetic hierarchy establishes antero-posterior patterning of esophagus striated muscle.
PF-04217903 purchased from AbMole
Nature. 2015 Jun 18;522(7556):349-53.
MET is required for the recruitment of anti-tumoural neutrophils.
PF-04217903 purchased from AbMole
Cell Experiment | |
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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 | |
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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 |
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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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Products are for research use only. Not for human use. We do not sell to patients.
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