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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
BioRxiv. 2019; .
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
-2[1].jpg) |
Source | Nature (2015). Figure 3. PF-04217903 and INCB28060 (AbMole Bioscience) |
| Method | mice treatment in vivo and histological evaluation | |
| Cell Lines | B16F10 cells | |
| Concentrations | 40mg/kg PF-04217903 and 50mg/kg INCB28060 | |
| Incubation Time | 2 weeks | |
| 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 . |
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Source | Nature (2015). Figure 2. PF-04217903 and INCB28060 (AbMole Bioscience) |
| Method | mice treatment in vivo and histological evaluation | |
| Cell Lines | B16F10 cells | |
| Concentrations | 40mg/kg PF-04217903 | |
| Incubation Time | 2 weeks | |
| 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." |
| 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 |
| 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. |
All AbMole products are for research use only, cannot be used for human consumption or veterinary use. We do not provide products or services to individuals. Please comply with the intended use and do not use AbMole products for any other purpose.
Products are for research use only. Not for human use. We do not sell to patients.
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