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$0.00 - Keisuke Enomoto, .et al. Synergistic Effects of Lenvatinib (E7080) and MEK Inhibitors against Anaplastic Thyroid Cancer in Preclinical Models, Cancers (Basel), 2021, Feb 18;13(4):862 PMID: 33670725
- Koide H, .et al. Substrate-dependent effects of molecular-targeted anticancer agents on activity of organic anion transporting polypeptide 1B1, Xenobiotica, 2018, Oct;48(10):1059-1071 PMID: 29034773
- Fujita KI, .et al. Involvement of the Transporters P-Glycoprotein and Breast Cancer Resistance Protein in Dermal Distribution of the Multikinase Inhibitor Regorafenib and Its Active Metabolites, J Pharm Sci, 2017, Sep;106(9):2632-2641 PMID: 28479358
- Tomoko Ogawa-Morita, .et al. Validation of a Liquid Chromatography-Tandem Mass Spectrometric Assay for Quantitative Analysis of Lenvatinib in Human Plasma, Int J Anal Chem, 2017, 2017: 2341876 PMID: 28680445
Biological Activity
E7080 is a multi-kinase inhibitor that inhibits both VEGFR2 and VEGFR3 kinases.
Targets
| Target | Value |
|---|---|
| VEGFR2/KDR | IC50: 4.0nM |
| VEGFR3/FLT4 | IC50: 5.2nM |
| VEGFR1/FLT1 | IC50: 22nM |
| PDGFRβ | IC50: 39nM |
| FGFR1 | IC50: 46nM |
| PDGFRα | IC50: 51nM |
| Kit | IC50: 100nM |
| EphB4 | IC50: >10μM |
| IGF-1R | IC50: >10μM |
| Insulin Receptor | IC50: >10μM |
| Src | IC50: >10μM |
| Akt1 | IC50: >10μM |
| CDK4/CyclinD | IC50: >10μM |
| PLK1 | IC50: >10μM |
| FAK | IC50: >10μM |
| PKCα | IC50: >10μM |
| In vitro (25°C) | DMSO | Warmed: 35 mg/mL (81.99 mM) | |
| Water | Insoluble | ||
| Ethanol | Insoluble | ||
| In vivo | 0.5% methylcellulose | 28 mg/mL | |
|
* <1 mg/ml means slightly soluble or insoluble. * Please note that Adooq tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations. |
|||
| Concentration / Solvent Volume / Mass | 1 mg | 5 mg | 10 mg |
|---|---|---|---|
| 0.1 mM | 23.42 mL | 117.12 mL | 234.25 mL |
| 0.5 mM | 4.68 mL | 23.42 mL | 46.85 mL |
| 1 mM | 2.34 mL | 11.71 mL | 23.42 mL |
| 5 mM | 0.47 mL | 2.34 mL | 4.68 mL |
*The above data is based on the productmolecular weight 426.9. Batch specific molecular weights may vary from batch to batch due to solvent of hydration, which will affect the solvent volumes required to prepare stock solutions.
| Catalog Num | A10340 |
|---|---|
| Actions | Inhibitor |
| CAS No. | 417716-92-8 |
| Formula | C21H19ClN4O4 |
| M. Wt | 426.9 |
| Purity | >98% |
| Synonyms | E-7080 |
| SMILES | COC1=CC2=NC=CC(=C2C=C1C(=O)N)OC3=CC(=C(C=C3)NC(=O)NC4CC4)Cl |
| Storage | Store lyophilized at -20ºC, keep desiccated. |
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