Target Selectivity of Axitinib (AG-013736)
| Key Target | IC50 | Description | Reference |
|---|---|---|---|
| VEGF receptor 1 | 0.1 nM | In vitro biochemical assay | PMC9101101 |
| VEGF receptor 3 | 0.1 nM | In vitro biochemical assay | PMC9101101 |
| VEGF receptor 2 | 0.2 nM | In vitro biochemical assay | PMC9101101 |
| VEGFR2 | 0.2 ng/ml | VEGFR2 autophosphorylation inhibition assay | PMC11426123 |
| Tie2 | 1.5 nM | Kinase HotSpot™ assay (IC93 determination) | PMC11149885 |
| cKIT V654A mutant | 4.56 nM | Biochemical enzymatic assay with [Vendor]'s SelectScreen technology | PMC6535728 |
| cKIT | 4.78 nM | Biochemical enzymatic assay with [Vendor]'s SelectScreen technology | PMC6535728 |
| cKIT N822K mutant | 9.12 nM | Biochemical enzymatic assay with [Vendor]'s SelectScreen technology | PMC6535728 |
| VEGFR-2 | 19 nM | Luminescence-based ADP-Glo™ kinase assay | PMC7734574 |
| cKIT T670I mutant | 51.8 nM | Biochemical enzymatic assay with [Vendor]'s SelectScreen technology | PMC6535728 |
| cKIT A829P mutant | 67.3 nM | Biochemical enzymatic assay with [Vendor]'s SelectScreen technology | PMC6535728 |
| cKIT D816H mutant | 68.6 nM | Biochemical enzymatic assay with [Vendor]'s SelectScreen technology | PMC6535728 |
| KDR/VEGFR2 | 260 nM | Radioisotopically-labeled ATP (33P-ɣ-ATP) reaction, quantified as percentage of remaining activity relative to vehicle controls, calculated using GraphPad Prism software. | PMC12679583 |
| cKIT D816V mutant | 1050 nM | Biochemical enzymatic assay with [Vendor]'s SelectScreen technology | PMC6535728 |
| Human liver microsomes | 10.63 μM | Microsome incubation assay, UPLC-MS/MS analysis, dose-response inhibition curve analysis by GraphPad Prism 5.0 software. | PMC9252588 |
| Rat liver microsomes | 15.76 μM | Microsome incubation assay, UPLC-MS/MS analysis, dose-response inhibition curve analysis by GraphPad Prism 5.0 software. | PMC9252588 |
Check the
Axitinib (AG-013736)
product page for in-depth specifications, including solubility, stock solutions, MOA, and working concentrations.
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- Axitinib (AG-013736) Mechanism of Action: VEGFR Inhibition in Tumor Endothelial Cells Research
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- Axitinib (AG-013736) Solubility in DMSO
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- Axitinib (AG-013736) Combination Database
- Axitinib (AG-013736) Molecular Weight
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- Axitinib (AG-013736) Chemical Structure (2D and 3D)
- Axitinib (AG-013736) IC50 for Cell-based and Cell-free Assays
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