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- 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
- Ellawatty WEA, .et al. Organic cation transporter 1 is responsible for hepatocellular uptake of the tyrosine kinase inhibitor pazopanib, Drug Metab Dispos, 2018, Jan;46(1):33-40 PMID: 29089306
- 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
Biological Activity
Pazopanib is a potent and selective multi-targeted receptor tyrosine kinase inhibitor of VEGFR-1, VEGFR-2, VEGFR-3, PDGFR-a/β, and c-kit that blocks tumor growth and inhibits angiogenesis.
Targets
| Target | Value |
|---|---|
| VEGFR1 | IC50: 10nM |
| VEGFR2 | IC50: 30nM |
| VEGFR3 | IC50: 47nM |
| FGFR | IC50: 74nM |
| PDGFR | IC50: 84nM |
| c-Kit | IC50: 140nM |
| c-Fms | IC50: 146nM |
| In vitro | DMSO | Warmed: 84 mg/mL (191.98 mM) | |
| Water | Insoluble | ||
| Ethanol | Insoluble | ||
|
* <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 | 22.86 mL | 114.29 mL | 228.57 mL |
| 0.5 mM | 4.57 mL | 22.86 mL | 45.71 mL |
| 1 mM | 2.29 mL | 11.43 mL | 22.86 mL |
| 5 mM | 0.46 mL | 2.29 mL | 4.57 mL |
*The above data is based on the productmolecular weight 437.5 . 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 | A11518 |
|---|---|
| Actions | Inhibitor |
| CAS No. | 444731-52-6 |
| Formula | C21H23N7O2S |
| M. Wt | 437.5 |
| Purity | >98% |
| Synonyms | GW 786034, Votrient,GW786034 |
| SMILES | CC1=C(C=C(C=C1)NC2=NC=CC(=N2)N(C)C3=CC4=NN(C(=C4C=C3)C)C)S(=O)(=O)N |
| Storage | Store lyophilized at -20ºC, keep desiccated. |
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