Regorafenib monohydrate |
| Catalog No.GC14534 |
A multi-kinase inhibitor
Products are for research use only. Not for human use. We do not sell to patients.
Cas No.: 1019206-88-2
Sample solution is provided at 25 µL, 10mM.
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Regorafenib monohydrate is a multitargetedinhibitor of tyrosine kinase with IC50 values of 13nM, 4.2nM, 46nM, 2.5nM, 28nM, 19nM, 202nM, 22nM, 7nM, 1.5nM and 311nM, respectively for VEGFR-1, mVEGFR-2, mVEGFR-3, Raf-1, BRAF WT, BRAFV600E, FGFR-1, PDGFR-β, c-KIT, RETand TIE2 [1].
Regorafenib is a multikinase inhibitor of both intracellular and membrane-bound RTKs. It shows potent inhibition of angiogenic and stromal RTKs like VEGF receptors-1-3, PDGFR-β and FGF receptor-1 with IC50 values ranging from4.2 to 311nM in biochemical assays. It also inhibits oncogenic RTKs, such as RET and c-KIT, with IC50 values ranging from 1.5 to 28nM in cellular assays [1].
Regorafenib is reported to have anti-tumor efficacy to various tumors including breast, pancreas, thyroid, melanoma, GIST, and CRC with a mean IC50 value less than 1μM. These inhibition effects of tumor growth are also found in mouse xenograft models after the treatment of regorafenib at dose ranging from 10 to 100 mg/kg [1].
References:
[1] Crona DJ, Keisler MD, Walko CM.Regorafenib: a novel multitargeted tyrosine kinase inhibitor for colorectal cancer and gastrointestinal stromal tumors.Ann Pharmacother. 2013 Dec;47(12):1685-96.
| Cell experiment [1]: | |
|
Cell lines |
Human umbilical vascular endothelial and human aortic smooth muscle cells |
|
Preparation method |
The solubility of this compound in DMSO is >25.1mg/mL. General tips for obtaining a higher concentration: Please warm the tube at 37℃ for 10 minutes and/or shake it in the ultrasonic bath for a while. Stock solution can be stored below -20℃ for several months. |
|
Reacting condition |
IC50: 2.6 and 146 nM |
|
Applications |
Regorafenib effectively inhibited proliferation of VEGF and FGF-2-stimulated human umbilical vascular endothelial and human aortic smooth muscle cells stimulated with the BB dimeric glycoprotein of PDGF with IC50 values of 2.6 and 146 nM, respectively. |
| Animal experiment [1]: | |
|
Animal models |
CRC, breast cancer, and renal cell carcinoma mouse xenograft models |
|
Dosage form |
10 to 100 mg/kg |
|
Application |
In CRC, breast cancer, and renal cell carcinoma mouse xenograft models, Regorafenib monohydrate inhibited tumor growth in a dose-dependent way. Regorafenib also decreased pERK1/2, suggesting that the antiproliferative effects of Regorafenib were through RAF/MEK/ERK signaling cascade inhibition. |
|
Other notes |
Please test the solubility of all compounds indoor, and the actual solubility may slightly differ with the theoretical value. This is caused by an experimental system error and it is normal. |
|
References: [1] Crona DJ, Keisler MD, Walko CM.Regorafenib: a novel multitargeted tyrosine kinase inhibitor for colorectal cancer and gastrointestinal stromal tumors.Ann Pharmacother. 2013 Dec;47(12):1685-96. | |
| Cas No. | 1019206-88-2 | SDF | |
| Chemical Name | 4-[4-[[4-chloro-3-(trifluoromethyl)phenyl]carbamoylamino]-3-fluorophenoxy]-N-methylpyridine-2-carboxamide;hydrate | ||
| 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.O | ||
| Formula | C21H17ClF4N4O4 | M.Wt | 500.83 |
| Solubility | ≥ 25.05 mg/mL in DMSO | Storage | Store 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. |
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| Shipping Condition | Evaluation sample solution: shipped with blue ice. All other sizes available: with RT, or with Blue Ice upon request. | ||
| Prepare stock solution | |||
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1 mg | 5 mg | 10 mg |
| 1 mM | 1.9967 mL | 9.9834 mL | 19.9669 mL |
| 5 mM | 0.3993 mL | 1.9967 mL | 3.9934 mL |
| 10 mM | 0.1997 mL | 0.9983 mL | 1.9967 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 ddH2O, 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: >99.50%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
- Datasheet
Average Rating: 5 (Based on Reviews and 30 reference(s) in Google Scholar.)
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