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$0.00 - Majid Momeny, .et al. Cediranib, an inhibitor of vascular endothelial growth factor receptor kinases, inhibits proliferation and invasion of prostate adenocarcinoma cells, Eur J Pharmacol, 2020, 882:173298
- Sunil Kumar Yadava, .et al. Low Temperature, Easy Scaling Up Method for Development of Smart Nanostructure Hybrid Lipid Capsules for Drug Delivery Application, Colloids Surf B Biointerfaces, 2020, Mar 2;190:110927 PMID: 32169777
- Takeshi Uenaka, .et al. In silico drug screening by using genome-wide association study data repurposed dabrafenib, an anti-melanoma drug, for Parkinson’s disease, Hum Mol Genet, 2018, Nov 15; 27(22): 3974-3985 PMID: 30137437
- Yi Xu, .et al. Knockdown of delta-5-desaturase promotes the anti-cancer activity of dihomo-γ-linolenic acid and enhances the efficacy of chemotherapy in colon cancer cells expressing COX-2, Free Radic Biol Med, 2016, Jul; 96: 67-77 PMID: 27101738 d
Biological Activity
Regorafenib (BAY 73-4506) is a multikinase inhibitor with IC50 of 17, 40 and 69 nM c-KIT, VEGFR2, B-Raf. Regorafenib (BAY 73-4506) is an orally bioavailable multikinase inhibitor targeting both the tumor and its vasculature.
Targets
| Target | Value |
|---|---|
| RET | IC50: 1.5nM |
| Raf-1 | IC50: 2.5nM |
| VEGFR2 | IC50: 4.2nM |
| Kit | IC50: 7nM |
| VEGFR1 | IC50: 13nM |
| B-Raf(V600E) | IC50: 19nM |
| PDGFRβ | IC50: 22nM |
| B-Raf | IC50: 28nM |
| VEGFR3 | IC50: 46nM |
| FGFR1 | IC50: 202nM |
| Tie-2 | IC50: 311nM |
| In vitro (25°C) | DMSO | 97 mg/mL (200.9 mM) | |
| Water | <1 mg/mL (<1 mM) | ||
| Ethanol | <1 mg/mL (<1 mM) | ||
| In vivo | 30% PEG400/0.5% Tween80/5% propylene glycol | 30 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 | 20.71 mL | 103.56 mL | 207.13 mL |
| 0.5 mM | 4.14 mL | 20.71 mL | 41.43 mL |
| 1 mM | 2.07 mL | 10.36 mL | 20.71 mL |
| 5 mM | 0.41 mL | 2.07 mL | 4.14 mL |
*The above data is based on the productmolecular weight 482.8. 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 | A10250 |
|---|---|
| Actions | Inhibitor |
| M. Wt | 482.8 |
| Formula | C21H15ClF4N4O3 |
| Solubility | DMSO |
| Purity | >98% |
| Storage | at -20°C 3 years Powder |
| CAS No. | 755037-03-7 |
| SMILES | CNC(=O)C1=NC=CC(=C1)OC2=CC(=C(C=C2)NC(=O)NC3=CC(=C(C=C3)Cl)C(F)(F)F)F |
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