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100mg | ||
250mg | ||
500mg |
ln Vitro |
In GIST 882, thyroid TT, MDA-MB-231, HepG2, A375, and SW620 cells, regorafenib mesylate (0–10 μM, 96 h) has anti-proliferative action [1]. In addition to inhibiting FGFR and pERK1/2, regorafenib mesylate (0-3000 nM, 30 minutes) also prevents VEGFR2, TIE2, and PDGFR-β from autophosphorylating[1]. Hep3B cell growth is inhibited by regorafenib mesylate in a concentration-dependent manner, with an IC50 of 5 μM. The JNK target phosphorylated c-Jun is then upregulated by regorafenib in Hep3B cells, but not total c-Jun [2].
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ln Vivo |
Regorafenib mesylate (10 mg/kg, PO, as a single dosage or daily for 4 days) reduces tumor vasculature and tumor development in the rat GS9L glioblastoma model [1]. Regorafenib mesylate (0-100 mg/kg, oral, qd × 9) demonstrates anti-tumor and anti-angiogenic actions in Colo-205, MDA-MB-231 and 786-O models [1].
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Cell Assay |
Cell Proliferation Assay[1]
Cell Types: GIST 882, Thyroid TT, MDA-MB-231, HepG2, A375 and SW620 Cell Tested Concentrations: 10 μM and 5 nM Incubation Duration: 96 hrs (hours) Experimental Results: In GIST 882, Thyroid TT, MDA- For MB-231, HepG2, A375 and SW620 cells, the IC50 values are 45 ± 20, 34 ± 8, 401 ± 88, 560 ± 200, 900, 967 ± 287 nM. respectively. Western Blot Analysis[1] Cell Types: NIH-3T3/VEGFR2 cells, (CHO)-TIE2 cells, HAoSMCs cells, MCF-7 cells Tested Concentrations: 0, 10, 30, 100, 300, 1000, 3000 nM Incubation Duration: 30 Minute Experimental Results: Inhibits autophosphorylation of VEGFR2, TIE2, and PDGFR-β with IC50 values of 3, 31, and 90 nM, respectively, inhibits FGFR signaling in FGF10-stimulated MCF-7 breast cancer (BC) cells, and shows inhibition Phosphorylates FGFR substrate 2 (pFRS2) and the downstream signaling kinase pERK1/2. |
Animal Protocol |
Animal/Disease Models: Rat GS9L glioblastoma xenograft[1]
Doses: 10 mg/kg Route of Administration: po (po (oral gavage)) single dose or one time/day for 4 days Experimental Results: Inhibition of rat GS9L glioblastoma Tumor vasculature and tumor growth in models. Animal/Disease Models: Female athymic NCr nu/nu (nude) mice, various xenograft models, including those derived from CRC (Colo-205), BC (MDA-MB-231) and RCC (786-O) tumors [1] Doses: 0, 3, 10, 30, 100 mg/kg Route of Administration: po (po (oral gavage)) qd × 9 Experimental Results: Effectively inhibited the growth of Colo-205, MDA-MB-231 and 786-O models. Dramatically reduces tumor MVA, effectively inhibits the RAF/MEK/ERK signaling cascade reaction, and Dramatically inhibits tumor cell proliferation. |
References |
[1]. Wilhelm SM, et al. Regorafenib (BAY 73-4506): a new oral multikinase inhibitor of angiogenic, stromal and oncogenic receptor tyrosine kinases with potent preclinical antitumor activity. Int J Cancer, 2011, 129(1), 245-255.
[2]. Carr BI, et al. Fluoro-Bay 43-9006 (Regorafenib) effects on hepatoma cells: growth inhibition, quiescence, and recovery. J Cell Physiol, 2013, 228(2), 292-297. |
Molecular Formula |
C21H15CLF4N4O3.CH4O3S
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Molecular Weight |
578.9211
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CAS # |
835621-08-4
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Related CAS # |
Regorafenib;755037-03-7;Regorafenib monohydrate;1019206-88-2;Regorafenib-d3;1255386-16-3
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Appearance |
Typically exists as solids (or liquids in special cases) at room temperature
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SMILES |
C1(C(NC)=O)=NC=CC(OC2=CC=C(NC(=O)NC3=CC=C(Cl)C(C(F)(F)F)=C3)C(F)=C2)=C1.S(C)(=O)(O)=O
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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) |
May dissolve in DMSO (in most cases), if not, try other solvents such as H2O, Ethanol, or DMF with a minute amount of products to avoid loss of samples
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Solubility (In Vivo) |
Note: Listed below are some common formulations that may be used to formulate products with low water solubility (e.g. < 1 mg/mL), you may test these formulations using a minute amount of products to avoid loss of samples.
Injection Formulations
Injection Formulation 1: DMSO : Tween 80: Saline = 10 : 5 : 85 (i.e. 100 μL DMSO stock solution → 50 μL Tween 80 → 850 μL Saline)(e.g. IP/IV/IM/SC) *Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH ₂ O to obtain a clear solution. Injection Formulation 2: DMSO : PEG300 :Tween 80 : Saline = 10 : 40 : 5 : 45 (i.e. 100 μL DMSO → 400 μLPEG300 → 50 μL Tween 80 → 450 μL Saline) Injection Formulation 3: DMSO : Corn oil = 10 : 90 (i.e. 100 μL DMSO → 900 μL Corn oil) Example: Take the Injection Formulation 3 (DMSO : Corn oil = 10 : 90) as an example, if 1 mL of 2.5 mg/mL working solution is to be prepared, you can take 100 μL 25 mg/mL DMSO stock solution and add to 900 μL corn oil, mix well to obtain a clear or suspension solution (2.5 mg/mL, ready for use in animals). View More
Injection Formulation 4: DMSO : 20% SBE-β-CD in saline = 10 : 90 [i.e. 100 μL DMSO → 900 μL (20% SBE-β-CD in saline)] Oral Formulations
Oral Formulation 1: Suspend in 0.5% CMC Na (carboxymethylcellulose sodium) Oral Formulation 2: Suspend in 0.5% Carboxymethyl cellulose Example: Take the Oral Formulation 1 (Suspend in 0.5% CMC Na) as an example, if 100 mL of 2.5 mg/mL working solution is to be prepared, you can first prepare 0.5% CMC Na solution by measuring 0.5 g CMC Na and dissolve it in 100 mL ddH2O to obtain a clear solution; then add 250 mg of the product to 100 mL 0.5% CMC Na solution, to make the suspension solution (2.5 mg/mL, ready for use in animals). View More
Oral Formulation 3: Dissolved in PEG400  (Please use freshly prepared in vivo formulations for optimal results.) |
Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
1 mM | 1.7274 mL | 8.6368 mL | 17.2735 mL | |
5 mM | 0.3455 mL | 1.7274 mL | 3.4547 mL | |
10 mM | 0.1727 mL | 0.8637 mL | 1.7274 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.