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- Paula Sagmeister, .et al. Comparative Response of HCC Cells to TKIs: Modified in vitro Testing and Descriptive Expression Analysis, J Hepatocell Carcinoma, 2022, Jul 9;9:595-607 PMID: 35845819
- Majid Momeny, .et al. Cediranib, a pan-inhibitor of vascular endothelial growth factor receptors, inhibits proliferation and enhances therapeutic sensitivity in glioblastoma cells, Life Sci, 2021, Dec 15;287:120100 PMID: 34715143
- Jindal A, .et al. Milciclib and sorafenib synergistically downregulate c-Myc to suppress tumor growth in an orthotopic murine model of human hepatocellular carcinoma, J Transl Sci, 2020, 7: 1-10
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- 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
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- 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
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 | 88 mg/mL (182.26 mM) | |
Water | Insoluble | ||
Ethanol | Insoluble | ||
In vivo | 2% DMSO+30% PEG 300+5% Tween 80+ddH2O | 4 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 |
CAS No. | 755037-03-7 |
Formula | C21H15ClF4N4O3 |
M. Wt | 482.8 |
Purity | >98% |
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 |
Storage | Store lyophilized at -20ºC, keep desiccated. |
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