2. Protein Tyrosine Kinase/RTK Autophagy MAPK/ERK Pathway
  3. VEGFR Autophagy PDGFR Raf RET FGFR c-Kit Tie
  4. Regorafenib monohydrate

Regorafenib monohydrate  (Synonyms: BAY 73-4506 monohydrate)

Cat. No.: HY-10331A Purity: 99.96%
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Regorafenib (BAY 73-4506) monohydrate is an orally active and potent multi-targeted receptor tyrosine kinase inhibitor, with IC50 values of 13/4.2/46, 22, 7, 1.5 and 2.5 nM for VEGFR1/2/3, PDGFRβ, Kit, RET and Raf-1, respectively. Regorafenib monohydrate shows very robust antitumor and antiangiogenic activity.

For research use only. We do not sell to patients.

Regorafenib monohydrate Chemical Structure

Regorafenib monohydrate Chemical Structure

CAS No. : 1019206-88-2

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Based on 61 publication(s) in Google Scholar

Other Forms of Regorafenib monohydrate:

Regorafenib monohydrate Related Antibodies

Top Publications Citing Use of Products

58 Publications Citing Use of MCE Regorafenib monohydrate

WB

    Regorafenib monohydrate purchased from MedChemExpress. Usage Cited in: Neoplasia. 2023 Mar 18;39:100897.  [Abstract]

    Regorafenib (0-40 µM; 36 h) markedly increases the expression of cleaved caspase-3, while decreases the expression of anti-apoptotic protein Bcl-2, in both H1299 and PC-9 cells.

    Regorafenib monohydrate purchased from MedChemExpress. Usage Cited in: Int J Mol Sci. 2018 Sep 25;19(10). pii: E2915.  [Abstract]

    Effects on the expression of phosphorylated extracellular signal-related kinase (p-ERK), ERK, thymidylate synthase (TS), and markers of cell death in SW620, HCT 116, and HT-29 cells using various Regorafenib treatment schedules.

    Regorafenib monohydrate purchased from MedChemExpress. Usage Cited in: Br J Cancer. 2017 Sep 26;117(7):974-983.  [Abstract]

    The effect of the AKT inhibitor MK2206 (10 μM) on the expression levels of phosphor-AKT, AKT, and STMN1 in TKI-pretreated NCI-H460 cells. β-actin is used as a loading control.

    View All VEGFR Isoform Specific Products:

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    VEGFR1/Flt-1 VEGFR2/KDR/Flk-1 VEGFR3/Flt-4

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    BRaf c-Raf Raf

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    FGFR FGFR1 FGFR2 FGFR3 FGFR4 FGF21

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    Tie2

    • Biological Activity

    • Purity & Documentation

    • References

    • Customer Review

    Description

    Regorafenib (BAY 73-4506) monohydrate is an orally active and potent multi-targeted receptor tyrosine kinase inhibitor, with IC50 values of 13/4.2/46, 22, 7, 1.5 and 2.5 nM for VEGFR1/2/3, PDGFRβ, Kit, RET and Raf-1, respectively. Regorafenib monohydrate shows very robust antitumor and antiangiogenic activity[1].

    IC50 & Target[1]

    Raf-1

    2.5 nM (IC50)

    Tie2

    311 ± 46 nM (IC50)

    VEGFR2

    4.2 nM (IC50)

    VEGFR1

    13 nM (IC50)

    BRafV600E

    19 nM (IC50)

    PDGFRβ

    22 nM (IC50)

    Braf

    28 nM (IC50)

    VEGFR3

    46 nM (IC50)

    In Vitro

    Regorafenib monohydrate (0-10 μM, 96 h) shows 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 the autophosphorylation of VEGFR2, TIE2 and PDGFR-β, and inhibits FGFR and pERK1/2[1].
    Regorafenib monohydrate causes a concentration-dependent decrease in Hep3B cell growth, with an IC50 of 5 μM. Regorafenib subsequently increases the levels of phospho-c-Jun, a JNK target, but not total c-Jun in Hep3B cells[3].

    MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

    Regorafenib monohydrate Related Antibodies

    Cell Proliferation Assay[1]

    Cell Line: GIST 882, Thyroid TT, MDA-MB-231, HepG2, A375 and SW620 cells
    Concentration: 10 μM and 5 nM
    Incubation Time: 96 h
    Result: Showed anti-proliferation activity in GIST 882, Thyroid TT, MDA-MB-231, HepG2, A375 and SW620 cells, with IC50 values of 45 ± 20, 34 ± 8, 401 ± 88, 560 ± 200, 900, 967 ± 287 nM. respectively.

    Western Blot Analysis[1]

    Cell Line: NIH-3T3/VEGFR2 cells, (CHO)-TIE2 cells, HAoSMCs cells, MCF-7 cells
    Concentration: 0, 10, 30, 100, 300, 1000, 3000 nM
    Incubation Time: 30 min
    Result: Inhibited the autophosphorylation of VEGFR2, TIE2 and PDGFR-β, with IC50 values of 3, 31, and 90 nM, respectively, inhibited FGFR signaling in MCF-7 breast cancer (BC) cells stimulated with FGF10, and showed inhibition of phosphorylated FGFR substrate 2 (pFRS2) and the downstream signaling kinase pERK1/2.
    In Vivo

    Regorafenib 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].
    Regorafenib 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].

    MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

    Animal Model: Rat GS9L glioblastoma xenograft[1]
    Dosage: 10 mg/kg
    Administration: Orally, single dose or daily for 4 days
    Result: Inhibited tumor vasculature and tumor growth in a rat GS9L glioblastoma model.
    Animal Model: Female athymic NCr nu/nu mice, Multiple xenograft models, including models derived from CRC (Colo-205), BC (MDA-MB-231) and RCC (786-O) tumors[1]
    Dosage: 0, 3, 10, 30, 100 mg/kg
    Administration: Orally, qd × 9
    Result: Effectively inhibited growth of the Colo-205, MDA-MB-231 and 786-O model. Significantly reduces tumor MVA, effectively inhibited the RAF/MEK/ERK signaling cascade, and drastically inhibited tumor cell proliferation.
    Clinical Trial
    Molecular Weight

    500.83

    Formula

    C21H17ClF4N4O4
    CAS No.
    Appearance

    Solid

    Color

    Light yellow to orange

    SMILES

    O=C(NC1=CC=C(C(C(F)(F)F)=C1)Cl)NC2=CC=C(OC3=CC(C(NC)=O)=NC=C3)C=C2F.O
    Shipping

    Room temperature in continental US; may vary elsewhere.
    Storage
    Powder -20°C 3 years
    4°C 2 years
    In solvent -80°C 2 years
    -20°C 1 year
    Solvent & Solubility
    In Vitro: 

    DMSO : 50 mg/mL (99.83 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

    Preparing
    Stock Solutions
    Concentration Solvent Mass 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
    View the Complete Stock Solution Preparation Table

    * Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
    Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.

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    Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

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    Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

    This equation is commonly abbreviated as: C1V1 = C2V2

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    In Vivo:

    Select the appropriate dissolution method based on your experimental animal and administration route.

    For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
    To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for in vivo experiments, it is recommended to prepare freshly and use it on the same day.
    The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.

    • Protocol 1

      Add each solvent one by one:  10% DMSO    40% PEG300    5% Tween-80    45% Saline

      Solubility: ≥ 2.5 mg/mL (4.99 mM); Clear solution

      This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).

      Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.

      Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
    • Protocol 2

      Add each solvent one by one:  10% DMSO    90% Corn Oil

      Solubility: ≥ 2.5 mg/mL (4.99 mM); Clear solution

      This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown). If the continuous dosing period exceeds half a month, please choose this protocol carefully.

      Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 900 μL Corn oil, and mix evenly.

    In Vivo Dissolution Calculator
    Please enter the basic information of animal experiments:

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    mg/kg

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    Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
    Please enter your animal formula composition:
    %
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    +
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    Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
    The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).
    Calculation results:
    Working solution concentration: mg/mL
    Method for preparing stock solution: mg drug dissolved in μL  DMSO (Stock solution concentration: mg/mL).
    The concentration of the stock solution you require exceeds the measured solubility. The following solution is for reference only. If necessary, please contact MedChemExpress (MCE).
    Method for preparing in vivo working solution for animal experiments: Take μL DMSO stock solution, add μL . μL , mix evenly, next add μL Tween 80, mix evenly, then add μL Saline.
     If the continuous dosing period exceeds half a month, please choose this protocol carefully.
    Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.
    Purity & Documentation

    Purity: 99.96%

    COA (246 KB) HNMR (172 KB) RP-HPLC (251 KB) LCMS (353 KB)

    Handling Instructions (2659 KB)
    References

    Complete Stock Solution Preparation Table

    * Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
    Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.

    Optional Solvent Concentration Solvent Mass 1 mg 5 mg 10 mg 25 mg
    DMSO 1 mM 1.9967 mL 9.9834 mL 19.9669 mL 49.9171 mL
    5 mM 0.3993 mL 1.9967 mL 3.9934 mL 9.9834 mL
    10 mM 0.1997 mL 0.9983 mL 1.9967 mL 4.9917 mL
    15 mM 0.1331 mL 0.6656 mL 1.3311 mL 3.3278 mL
    20 mM 0.0998 mL 0.4992 mL 0.9983 mL 2.4959 mL
    25 mM 0.0799 mL 0.3993 mL 0.7987 mL 1.9967 mL
    30 mM 0.0666 mL 0.3328 mL 0.6656 mL 1.6639 mL
    40 mM 0.0499 mL 0.2496 mL 0.4992 mL 1.2479 mL
    50 mM 0.0399 mL 0.1997 mL 0.3993 mL 0.9983 mL
    60 mM 0.0333 mL 0.1664 mL 0.3328 mL 0.8320 mL
    80 mM 0.0250 mL 0.1248 mL 0.2496 mL 0.6240 mL
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    Regorafenib monohydrate Related Classifications

    Help & FAQs
    • Do most proteins show cross-species activity?

      Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

    Keywords:

    Regorafenib1019206-88-2BAY 73-4506VEGFRAutophagyPDGFRRafRETFGFRc-KitTieVascular endothelial growth factor receptorPlatelet-derived growth factor receptorRaf kinasesFibroblast growth factor receptorSCFRCD117Angiopoietin receptorAntitumorigenicantiangiogenictumorHUVECsHep3B cellHAoSMCsNIH-3T3Colo-205MDA-MB-231786-OInhibitorinhibitorinhibit

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