Regorafenib (Synonyms: BAY 73-4506) |
Catalog No.GC10111
One-Click Copy Product Info
|
Regorafenib is an orally active multi-kinase inhibitor with IC50 values of 13/4.2/46, 22, 7, 1.5 and 2.5nM for VEGFR1/2/3, PDGFRβ, Kit, RET and Raf-1, respectively.
Products are for research use only. Not for human use. We do not sell to patients.
Cas No.: 755037-03-7
Sample solution is provided at 25 µL, 10mM.
Regorafenib is an orally active multi-kinase inhibitor with IC50 values of 13/4.2/46, 22, 7, 1.5 and 2.5nM for VEGFR1/2/3, PDGFRβ, Kit, RET and Raf-1, respectively[1]. Regorafenib has good anti-tumor and anti-angiogenic activities[2, 3].
In vitro, Regorafenib (0-20μM) treatment of lung squamous cell carcinoma (LSCC) cell lines (NCI-H1703, NCI-H2170, SK-MES-1 cells) for 24-72h, inhibited cell proliferation in a dose- and time-dependent manner and induced cell G0/G1 phase arrest[4]. Regorafenib (2.5-10μM) treatment of HepG2 cells for 24-96h, inhibited cell growth in a dose- and time-dependent manner, induced cell apoptosis, and increased the level of phosphorylated c-Jun[5].
In vivo, oral treatment of mice with adrenal SK-N-SH neuroblastoma orthotopically implanted with Regorafenib (30mg/kg) for 14 days, significantly inhibited tumor growth in the mice, with the average final weight of the tumor in the control group being 2.16g and the average final weight of the tumor in the Regorafenib-treated group being only 0.35g[6]. Oral treatment of mice with metastatic colon cancer model with Regorafenib (30mg/kg) for 14 days, inhibited tumor growth and metastasis in the mice, significantly reduced tumor angiogenesis, and significantly reduced the number of infiltrating macrophages[7].
References:
[1] Wilhelm S M, Dumas J, Adnane L, et al. Regorafenib (BAY 73‐4506): a new oral multikinase inhibitor of angiogenic, stromal and oncogenic receptor tyrosine kinases with potent preclinical antitumor activity[J]. International journal of cancer, 2011, 129(1): 245-255.
[2] Chen C H, Hsu F T, Chen W L, et al. Induction of apoptosis, inhibition of MCL-1, and VEGF-A expression are associated with the anti-cancer efficacy of magnolol combined with regorafenib in hepatocellular carcinoma[J]. Cancers, 2021, 13(9): 2066.
[3] Lim Y, Han S W, Yoon J H, et al. Clinical implication of anti-angiogenic effect of regorafenib in metastatic colorectal cancer[J]. PLoS One, 2015, 10(12): e0145004.
[4] Hu X, Wu L, Zhang Z, et al. The anti-tumor effect of regorafenib in lung squamous cell carcinoma in vitro[J]. Biochemical and Biophysical Research Communications, 2018, 503(2): 1123-1129.
[5] Carr B I, Cavallini A, Lippolis C, et al. Fluoro‐Sorafenib (Regorafenib) effects on hepatoma cells: growth inhibition, quiescence, and recovery[J]. Journal of cellular physiology, 2013, 228(2): 292-297.
[6] Subramonian D, Phanhthilath N, Rinehardt H, et al. Regorafenib is effective against neuroblastoma in vitro and in vivo and inhibits the RAS/MAPK, PI3K/Akt/mTOR and Fos/Jun pathways[J]. British journal of cancer, 2020, 123(4): 568-579.
[7] Abou-Elkacem L, Arns S, Brix G, et al. Regorafenib inhibits growth, angiogenesis, and metastasis in a highly aggressive, orthotopic colon cancer model[J]. Molecular cancer therapeutics, 2013, 12(7): 1322-1331.
| Cell experiment [1]: | |
|
Cell lines |
NCI-H1703, NCI-H2170, SK-MES-1 cells |
|
Preparation Method |
Lung squamous cell carcinoma (LSCC) cell lines were exposed to different concentrations of Regorafenib for 24, 48, and 72h, 0-5μM for NCI-H1703 and 0-20μM for NCI-H2170 and SK-MES-1. Cell proliferation was measured by SRB assay. |
|
Reaction Conditions |
0-20μM; 24, 48, 72h |
|
Applications |
Regorafenib decreased the survival fractions of LSCC cells in a dose- and time-dependent manner. |
| Animal experiment [2]: | |
|
Animal models |
Female athymic nu/nu mice |
|
Preparation Method |
Mice with orthotopic adrenal SK-N-SH neuroblastoma xenograft tumours were treated with vehicle or Regorafenib. Mice in group 1 were gavage-fed once daily with vehicle alone, while the other group of mice was fed once daily with Regorafenib at 30mg/kg. Both groups of mice were treated for 14 days and then euthanised by CO2 followed by cervical dislocation. Tumours were harvested, weighed and photographed. |
|
Dosage form |
30mg/kg; 14 days; p.o. |
|
Applications |
Regorafenib reduces xenograft tumour growth. The average final weight of the tumors in the control group was 2.16g, while the average final weight of the tumors in the Regorafenib-treated group was only 0.35g. |
|
References: |
|
| Cas No. | 755037-03-7 | SDF | |
| Synonyms | BAY 73-4506 | ||
| Chemical Name | 4-(4-(3-(4-chloro-3-(trifluoromethyl)phenyl)ureido)-3-fluorophenoxy)-N-methylpicolinamide | ||
| Canonical 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 | ||
| Formula | C21H15ClF4N4O3 | M.Wt | 482.82 |
| Solubility | ≥100mg/mL in DMSO | Storage | Desiccate at -20°C |
| General tips | Please select the appropriate solvent to prepare the stock solution according to the
solubility of the product in different solvents; once the solution is prepared, please store it in
separate packages to avoid product failure caused by repeated freezing and thawing.Storage method
and period of the stock solution: When stored at -80°C, please use it within 6 months; when stored
at -20°C, please use it within 1 month. To increase solubility, heat the tube to 37°C and then oscillate in an ultrasonic bath for some time. |
||
| Shipping Condition | Evaluation sample solution: shipped with blue ice. All other sizes available: with RT, or with Blue Ice upon request. | ||
| Prepare stock solution | |||
|
1 mg | 5 mg | 10 mg |
| 1 mM | 2.0712 mL | 10.3558 mL | 20.7117 mL |
| 5 mM | 414.2 μL | 2.0712 mL | 4.1423 mL |
| 10 mM | 207.1 μL | 1.0356 mL | 2.0712 mL |
Step 1: Enter information below (Recommended: An additional animal making an allowance for loss during the experiment)
g
μL
Step 2: Enter the in vivo formulation (This is only the calculator, not formulation. Please contact us first if there is no in vivo formulation at the solubility Section.)
Calculation results:
Working concentration: mg/ml;
Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid concentration mg/mL, Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug. )
Method for preparing in vivo formulation: Take μL DMSO master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL saline, mix and clarify.
Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.
Note: 1. Please make sure the liquid is clear before adding the next solvent.
2. Be sure to add the solvent(s) in order. You must ensure that the solution obtained, in the previous addition, is a clear solution before proceeding to add the next solvent. Physical methods such as vortex, ultrasound or hot water bath can be used to aid dissolving.
3. All of the above co-solvents are available for purchase on the GlpBio website.
Quality Control & SDS
- View current batch:
- Purity: >99.00% Appearance: A solid
- COA (Certificate of Analysis)
- SDS (Safety Data Sheet)
- Datasheet
Average Rating: 5 (Based on Reviews and 30 reference(s) in Google Scholar.)