| Size | Price | Stock | Qty |
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| 10mg |
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| 50mg |
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| 100mg |
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| 250mg |
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| 500mg |
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Regorafenib monohydrate (also known as BAY 73-4506 monohydrate), the hydrated form of Regorafenib, is an orally bioavailable multi-kinase inhibitor targeting kinases such as VEGFR1, VEGFR2, VEGFR3, PDGFRβ, Kit, RET and Raf-1 with IC50 values of 13 nM/4.2 nM/46 nM, 22 nM, 7 nM, 1.5 nM and 2.5 nM in cell-free assays, respectively. IIt has anticancer properties and has received FDA approval for the management of liver cancer.
| Targets |
Raf-1 (IC50 = 2.5 nM); Tie2 (IC50 = 311 ± 46 nM); VEGFR2 (IC50 = 4.2 nM); VEGFR1 (IC50 = 13 nM); BRafV600E (IC50 = 19 nM); PDGFRβ (IC50 = 22 nM); Braf (IC50 = 28 nM); VEGFR3 (IC50 = 46 nM)
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| ln Vitro |
Regorafenib monohydrate (0–10 μM, 96 h) exhibits anti-proliferation activity in GIST 882, Thyroid TT, MDA-MB-231, HepG2, A375, and SW620 cells[1].
Regorafenib monohydrate (0–3000 nM, 30 min) inhibits FGFR and pERK1/2 as well as VEGFR2, TIE2, and PDGFR– autophosphorylation[1]. Regorafenib monohydrate has an IC50 of 5 μM and inhibits Hep3B cell growth in a concentration-dependent manner. Regorafenib then elevates phospho-c-Jun levels in Hep3B cells, a JNK target, but not total c-Jun levels[3]. |
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| ln Vivo |
Rogafenib monohydrate (10 mg/kg, Orally, single dose or daily for 4 days) inhibits tumor vasculature and tumor growth in a rat GS9L glioblastoma model[1].
Rogafenib monohydrate (0-100 mg/kg, Orally, qd × 9) exhibits antitumorigenic and antiangiogenic effects in the Colo-205, MDA-MB-231, and 786-O model[1]. |
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| Enzyme Assay |
Raf-1 (aa305-aa648), PDGFRβ (aa561-aa1106), VEGFR2 (murine aa785-aa1367), VEGFR3 (murine aa818-aa1363), and BRafV600E (aa409-aa765) kinase domains are used in in vitro tests. An initial 1 μM Regorafenib concentration is used for in vitro kinase inhibition profiling. Selected responding kinases, such as VEGFR1 and RET, are used to determine the IC50 values, which stand for the inhibitory concentration of 50%. By using a recombinant fusion protein of glutathione-S-transferase, the intracellular domain of TIE2, and the peptide biotin-Ahx-EPKDDAYPLYSDFG as substrate, the homogeneous time-resolved fluorescence (HTRF) assay is used to measure TIE2 kinase inhibition.
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| Cell Assay |
GIST 882 and TT cells are grown in RPMI medium with L-glutamine for proliferation assays, while MDA-MB-231, HepG2, and A375 cells are grown in DMEM that is always supplemented with 10% hiFBS. Trypsinized cells are plated at a density of 5 104 cells per well in 96-well plates containing complete media containing 10% FBS, and grown overnight at 37 °C. The following day, vehicle or regorafenib is added, serially diluted in complete growth media to final concentrations between 10 M and 5 nM, along with 0.2% DMSO, and the incubation is continued for another 96 hours. Quantifying cell proliferation.
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| Animal Protocol |
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| References |
| Molecular Formula |
C₂₁H₁₇CLF₄N₄O₄
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|---|---|
| Molecular Weight |
500.83
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| Exact Mass |
500.09
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| Elemental Analysis |
C, 50.36; H, 3.42; Cl, 7.08; F, 15.17; N, 11.19; O, 12.78
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| CAS # |
1019206-88-2
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| Related CAS # |
Regorafenib;755037-03-7;Regorafenib Hydrochloride;835621-07-3;Regorafenib mesylate;835621-08-4
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| Appearance |
Solid powder
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| 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
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| InChi Key |
ZOPOQLDXFHBOIH-UHFFFAOYSA-N
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| InChi Code |
InChI=1S/C21H15ClF4N4O3.H2O/c1-27-19(31)18-10-13(6-7-28-18)33-12-3-5-17(16(23)9-12)30-20(32)29-11-2-4-15(22)14(8-11)21(24,25)26;/h2-10H,1H3,(H,27,31)(H2,29,30,32);1H2
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| Chemical Name |
4-[4-[[4-chloro-3-(trifluoromethyl)phenyl]carbamoylamino]-3-fluorophenoxy]-N-methylpyridine-2-carboxamide;hydrate
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| Synonyms |
BAY-734506 monohydratel; BAY 734506; BAY734506; Regorafenib HCl. Brand name: Stivarga
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| HS Tariff Code |
2934.99.9001
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| Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month |
| Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
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| Solubility (In Vitro) |
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| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.5 mg/mL (4.99 mM) (saturation unknown) in 10% DMSO + 40% PEG300 + 5% Tween80 + 45% Saline (add these co-solvents sequentially from left to right, and one by one), clear solution.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 25.0 mg/mL clear DMSO stock solution to 400 μL PEG300 and mix evenly; then add 50 μL Tween-80 to the above solution and mix evenly; then add 450 μL normal saline to adjust the volume to 1 mL. Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH₂ O to obtain a clear solution. Solubility in Formulation 2: ≥ 2.5 mg/mL (4.99 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one), clear solution. For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 25.0 mg/mL clear DMSO stock solution to 900 μL of corn oil and mix evenly. View More
Solubility in Formulation 3: 30% PEG400+0.5% Tween80+5% Propylene glycol : 30mg/mL |
| Preparing Stock Solutions | 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 |
*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.
Calculation results
Working concentration： mg/mL；
Method for preparing DMSO stock solution： mg drug pre-dissolved in μL DMSO (stock solution 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 stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O，mix and clarify.
(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
(2) Be sure to add the solvent(s) in order.
| NCT Number | Recruitment | interventions | Conditions | Sponsor/Collaborators | Start Date | Phases |
| NCT03878524 | Active Recruiting |
Drug: Afatinib Drug: Regorafenib |
Metastatic Breast Carcinoma Anemia |
OHSU Knight Cancer Institute | April 1, 2020 | Phase 1 |
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Regorafenib inhibits key kinase targets in cells expressing VEGFR2, TIE2, PDGFR‐β, or FGFR.Int J Cancer.2011 Jul 1;129(1):245-55. |
Regorafenib inhibits tumor vasculature and tumor growth in a rat GS9L glioblastoma model: time‐course analysis by DCE‐MRI.Int J Cancer.2011 Jul 1;129(1):245-55. |
Regorafenib significantly reduces tumor MVA in the Colo‐205 CRC xenograft model.Int J Cancer.2011 Jul 1;129(1):245-55. |
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Regorafenib exhibits antitumorigenic and antiangiogenic effects in the MDA‐MB‐231 breast xenograft model.Int J Cancer.2011 Jul 1;129(1):245-55. |
In vivoantitumor efficacy of regorafenib.Int J Cancer.2011 Jul 1;129(1):245-55. |
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