Cell-free Assays (IC50/Ki) for Axitinib (AG-013736)
| Key Target | IC50 (Cell-free) | Description | Reference |
|---|---|---|---|
| VEGFR2 | 0.2 ng/ml | VEGFR2 autophosphorylation inhibition assay | PMC11426123 |
| 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. | Download PDF |
| Tie2 | 1.5nM | Kinase HotSpot™ assay (IC93 determination) | Download PDF |
| VEGF receptor 1 | 0.1 nM | In vitro biochemical assay | Download PDF |
| VEGF receptor 2 | 0.2 nM | In vitro biochemical assay | Download PDF |
| VEGF receptor 3 | 0.1–0.3 nM | In vitro biochemical assay | Download PDF |
| 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 |
| VEGFR2 | 0.5 nM (0.2 ng/mL) | VEGFR2 autophosphorylation inhibition assay | PMC8212425 |
| VEGFR-2 kinase | 19 nM | Luminescence-based ADP-Glo™ kinase assay | Download PDF |
| cKIT wild type | 4.78 nM | Biochemical enzymatic assay with [Vendor]'s SelectScreen technology | PMC6535728 |
| cKIT V654A mutant | 4.56 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 |
| 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 |
| cKIT D816V mutant | 1050 nM | Biochemical enzymatic assay with [Vendor]'s SelectScreen technology | PMC6535728 |
Cell-based Assay (IC50) for Axitinib (AG-013736)
| Cell Type | IC50 (Cell-based) | Description | Reference |
|---|---|---|---|
| MCF-7 | 1.1 µM | WST-1 assay | Download PDF |
| A549 | 2.0 µM | Cell Counting Kit-8 (CCK-8) assay | Download PDF |
| PC9 | 5 µM | Cell Counting Kit-8 (CCK-8) assay | Download PDF |
| HeLa cells (wild-type) | 2 nM | Determination of drug concentration inhibiting half of the induced PDGFRβ phosphorylation using ELISA and immunoblot analysis. | PMC10631511 |
| SNU-228 control cells | >20μM | Cell viability measurement using EZ-CYTOX assay and calculation of IC50 based on cell population. | Download PDF |
| SNU-228 sunitinib-resistant cells | 6.33μM | Cell viability measurement using EZ-CYTOX assay and calculation of IC50 based on cell population. | Download PDF |
| SNU-228 reversible cells | 15.67μM | Cell viability measurement using EZ-CYTOX assay and calculation of IC50 based on cell population. | Download PDF |
| SNU-267 control cells | 7.49μM | Cell viability measurement using EZ-CYTOX assay and calculation of IC50 based on cell population. | Download PDF |
| SNU-267 sunitinib-resistant cells | 1.5μM | Cell viability measurement using EZ-CYTOX assay and calculation of IC50 based on cell population. | Download PDF |
| SNU-267 reversible cells | 1.93μM | Cell viability measurement using EZ-CYTOX assay and calculation of IC50 based on cell population. | Download PDF |
| DAOY | 2.3 ± 1.5 µM | MTT colorimetric assay, calculated using the nonlinear regression method of Prism 5 software | Download PDF |
| HD-MB03 | 0.47 ± 0.2 µM | MTT colorimetric assay, calculated using the nonlinear regression method of Prism 5 software | Download PDF |
| D458 | 0.49 ± 0.4 µM | MTT colorimetric assay, calculated using the nonlinear regression method of Prism 5 software | Download PDF |
| CHLA-01-Med | 3.9 ± 0.23 µM | MTT colorimetric assay, calculated using the nonlinear regression method of Prism 5 software | Download PDF |
| HDF | >100 µM | MTT colorimetric assay, calculated using the nonlinear regression method of Prism 5 software | Download PDF |
| C8-D1A | >100 µM | MTT colorimetric assay, calculated using the nonlinear regression method of Prism 5 software | Download PDF |
| A-498 | 13.6 µM | MTT assay | Download PDF |
| Caki-2 | 36 µM | MTT assay | Download PDF |
| Ba/F3 (cKIT wild type) | 50 nM | Cell Titer-Glo assay | PMC6535728 |
| Ba/F3 (T670I mutant) | 108 nM | Cell Titer-Glo assay | PMC6535728 |
| Ba/F3 (T670I/V559D mutant) | 191 nM | Cell Titer-Glo assay | PMC6535728 |
| Ba/F3 (V654A mutant) | 5 nM | Cell Titer-Glo assay | PMC6535728 |
| Ba/F3 (V654A/V559D mutant) | 20 nM | Cell Titer-Glo assay | PMC6535728 |
| GIST-T1 | 21 nM | Cell Titer-Glo assay | PMC6535728 |
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) Working Concentration | Cell Culture | Treatment
- Axitinib (AG-013736) Solubility in DMSO
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- Axitinib (AG-013736) Combination Database
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