2. MAPK/ERK Pathway Protein Tyrosine Kinase/RTK Autophagy Apoptosis
  3. Raf VEGFR FLT3 Autophagy Ferroptosis Apoptosis
  4. Sorafenib Tosylate

Sorafenib Tosylate  (Synonyms: Bay 43-9006 Tosylate)

Cat. No.: HY-10201A Purity: 99.91%
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Sorafenib Tosylate (Bay 43-9006 Tosylate) is a potent and orally active Raf inhibitor with IC50s of 6 nM and 20 nM for Raf-1 and B-Raf, respectively. SorafenibTosylate is a multikinase inhibitor with IC50s of 90 nM, 15 nM, 20 nM, 57 nM and 58 nM for VEGFR2, VEGFR3, PDGFRβ, FLT3 and c-Kit, respectively. Sorafenib Tosylate induces autophagy and apoptosis. Sorafenib Tosylate has anti-tumor activity. Sorafenib Tosylate is a ferroptosis activator.

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

Sorafenib Tosylate Chemical Structure

Sorafenib Tosylate Chemical Structure

CAS No. : 475207-59-1

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Solid + Solvent (Highly Recommended)
10 mM * 1 mL in DMSO
ready for reconstitution
 USD 73 In-stock
Solution
10 mM * 1 mL in DMSO USD 73 In-stock
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500 mg USD 86 In-stock
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Based on 200 publication(s) in Google Scholar

Other Forms of Sorafenib Tosylate:

Sorafenib Tosylate Related Antibodies

Top Publications Citing Use of Products

188 Publications Citing Use of MCE Sorafenib Tosylate

RT-PCR
WB
Cell Viability Assay
Proliferation Assay

    Sorafenib Tosylate purchased from MedChemExpress. Usage Cited in: Discov Oncol. 2023 May 27;14(1):83.  [Abstract]

    Sorafenib (3 µM; 24 h) significantly inhibits the cell proliferation of HepG2 and Hep3B.

    Sorafenib Tosylate purchased from MedChemExpress. Usage Cited in: Discov Oncol. 2023 May 27;14(1):83.  [Abstract]

    Sorafenib (0.25, 0.5, 1, 2, 4, 6 µM; 24 h) significantly inhibits the cell viability of HepG2 and Hep3B.

    Sorafenib Tosylate purchased from MedChemExpress. Usage Cited in: Int J Biol Sci. 2018 Apr 25;14(5):577-585.  [Abstract]

    Hep3B, HepG2 and Huh7 cells are treated with 5 μM Sorafenib. The expressing levels of JAK1, JAK2, STAT3, SHP1, SHP2, actin and phosphorylation levels of STAT3 are determined by western blot using the antibodies, respectively.

    Sorafenib Tosylate purchased from MedChemExpress. Usage Cited in: Oncol Rep. 2018 Sep;40(3):1525-1532.  [Abstract]

    SMMC-7721 and HepG2 cells are treated with 4 µM Sorafenib and 100 µM Berberine alone or in combination (4 µM Sorafenib+100 µM Berberine) for 72 h, and the expression levels of apoptosis-associated proteins are measured by western blot analysis.

    Sorafenib Tosylate 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.

    Sorafenib Tosylate purchased from MedChemExpress. Usage Cited in: Am J Cancer Res. 2017 Dec 1;7(12):2503-2514.  [Abstract]

    VPA potentiates anti-tumor effects of Sorafenib tosylate in vivo. The expression of cleaved caspase9, cleaved caspase3, cleaved PARP from tumor tissue homogenates are analyzed by western blot.

    Sorafenib Tosylate purchased from MedChemExpress. Usage Cited in: J Pharmacol Exp Ther. 2017 Aug;362(2):219-229.  [Abstract]

    The combination of sorafenib and CAI induces apoptosis in NSCLC. Effect of 10 μM CAI and/or 5 μM Sorafenib on the expression of cleaved PARP and cleaved caspase-. Protein levels of cleaved PARP and cleaved caspase-3 from treated cell lysates are normalized against GAPDH levels.

    Sorafenib Tosylate purchased from MedChemExpress. Usage Cited in: Endocr J. 2017 Nov 29;64(11):1115-1123.  [Abstract]

    Effect of Sorafenib and Forskolin on expression of CDK4 and CDK regulatory proteins. Thyroid cancer cells are treated for 24 hours with 10 μM Sorafenib, 10 μM Forskolin, and combination therapy of 10 μM Sorafenib with 10 μM Forskolin. The expression of cyclin D1, CDK4, and phosphorylation of RB are examined by immunoblot analysis. β-actin is used as the control. The combination therapy suppresses expression of cyclin D1, and Forskolin monotherapy suppresses expression of cyclin D1 in TPC-1 and W

    Sorafenib Tosylate purchased from MedChemExpress. Usage Cited in: Endocr J. 2017 Nov 29;64(11):1115-1123.  [Abstract]

    Effect of Sorafenib on phosphorylation of ERK and AKT. Thyroid cancer cells are treated for 30 minutes with 10 μM Sorafenib, 10 μM Forskolin, and combination therapy of 10 μM Sorafenib with 10 μM Forskolin. The levels of ERK and AKT phosphorylation are examined by immunoblot analysis. β-actin is used as the control. Sorafenib suppresses phosphorylation of ERK, but not of AKT.

    Sorafenib Tosylate purchased from MedChemExpress. Usage Cited in: Oncotarget. 2017 May 2;8(18):29771-29784.  [Abstract]

    Sorafenib inhibits Pin1 biosynthesis and accumulation in Huh7 and HepG2 cells. Cells are treated with 5 or 10 μM Sorafenib for indicated times. Pin1 protein expression is determined by Western Blot.

    Sorafenib Tosylate purchased from MedChemExpress. Usage Cited in: Int J Clin Exp Pathol. 2015 Apr 1;8(4):3871-81.  [Abstract]

    The relationship between SOX9 and Raf/MEK/ERK signaling pathway. Co-treatment of si-SOX9-1 and Sorafenib (10uM, 15uM)/SU 11248 (2 uM, 3 uM) significantly decreases expression of MEK1 and its phosphorylated protein (p-MEK1/2, p-ERK1/2) as assayed by RT-PCR (with β-actin as internal control).

    Sorafenib Tosylate purchased from MedChemExpress. Usage Cited in: Int J Clin Exp Pathol. 2015 Apr 1;8(4):3871-81.  [Abstract]

    The relationship between SOX9 and Raf/MEK/ERK signaling pathway. Co-treatment of si-SOX9-1 and Sorafenib (10uM, 15uM)/SU 11248 (2 uM, 3 uM) significantly decreases expression of MEK1 and its phosphorylated protein (p-MEK1/2, p-ERK1/2) as assayed by Western blot (with GAPDH as internal control).

    View All Raf Isoform Specific Products:

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    BRaf c-Raf Raf

    View All VEGFR Isoform Specific Products:

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

    • Biological Activity

    • Protocol

    • Purity & Documentation

    • References

    • Customer Review

    Description

    Sorafenib Tosylate (Bay 43-9006 Tosylate) is a potent and orally active Raf inhibitor with IC50s of 6 nM and 20 nM for Raf-1 and B-Raf, respectively. SorafenibTosylate is a multikinase inhibitor with IC50s of 90 nM, 15 nM, 20 nM, 57 nM and 58 nM for VEGFR2, VEGFR3, PDGFRβ, FLT3 and c-Kit, respectively. Sorafenib Tosylate induces autophagy and apoptosis. Sorafenib Tosylate has anti-tumor activity. Sorafenib Tosylate is a ferroptosis activator[1].

    IC50 & Target[1]

    VEGFR3

    20 nM (IC50)

    Braf

    22 nM (IC50)

    Raf-1

    6 nM (IC50)

    VEGFR2

    90 nM (IC50)

    BrafV599E

    38 nM (IC50)

    PDGFRβ

    57 nM (IC50)

    c-Kit

    68 nM (IC50)

    Flt3

    58 nM (IC50)

    In Vitro

    Sorafenib Tosylate also inhibits BRAFwt (IC50=22 nM), BRAFV599E (IC50=38 nM), VEGFR-2 (IC50=90 nM), VEGFR-3 (IC50=20 nM), PDGFR-β (IC50=57 nM), c-KIT (IC50=68 nM), and Flt3 (IC50=58 nM) in biochemical assays[1].
    Sorafenib Tosylate-induced phosphorylation of c-Met, p70S6K and 4EBP1 is significantly reduced when 10-0505 cells are co-treated with anti-human anti-HGF antibody, suggesting that treatment with Sorafenib Tosylate leads to increased HGF secretion and activation of c-Met and mTOR targets[2].

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

    Sorafenib Tosylate Related Antibodies
    In Vivo

    Sorafenib Tosylate (10, 30, 50 and 100 mg/kg, orally) treatment inhibits the tumor growth of 06-0606 and 10-0505 xenografts in a dose-dependent manner (P<0.01). The growth rate of 06-0606 and 10-0505 xenografts is also significantly reduced by Sorafenib. The weights of 06-0606 tumors in mice that are treated with Sorafenib 50 mg/kg and 100 mg/kg are approximately 13% and 5% of the controls, respectively. 50 mg dose of Sorafenib significantly inhibits tumor growth in mice with lines 5-1318, 26-1004 and 10-0505 (P<0.01). For 50 mg dose, the T/C ratio, where T and C are the median weight (mg) of Sorafenib- and vehicle-treated tumors at the end of the treatment, respectively, for 06-0606, 26-1004, 5-1318, and 10-0505 xenografts is 0.13, 0.10, 0.12 and 0.49, respectively[2]. The survival rate is 73.3 % in Diethyl nitrosamine (DENA) group and 83.3 % in Sorafenib group compared to 100 % in the normal control group. DENA group shows a significant increase in liver index (1.51-fold increase, p<0.05) compared to normal control group, while treatment with Sorafenib shows significant decrease (p<0.05) in liver index when compared to DENA group. The liver index in Sorafenib group significantly decreases to lower than its value in the normal control[3].

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

    637.03

    Formula

    C28H24ClF3N4O6S
    CAS No.
    Appearance

    Solid

    Color

    White to off-white

    SMILES

    O=S(C1=CC=C(C=C1)C)(O)=O.O=C(NC2=CC=C(C(C(F)(F)F)=C2)Cl)NC3=CC=C(OC4=CC(C(NC)=O)=NC=C4)C=C3
    Shipping

    Room temperature in continental US; may vary elsewhere.
    Storage

    4°C, sealed storage, away from moisture

    *In solvent : -80°C, 1 year; -20°C, 6 months (sealed storage, away from moisture)

    Solvent & Solubility
    In Vitro: 

    DMSO : ≥ 31 mg/mL (48.66 mM; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

    *"≥" means soluble, but saturation unknown.

    Preparing
    Stock Solutions
    Concentration Solvent Mass 1 mg 5 mg 10 mg
    1 mM 1.5698 mL 7.8489 mL 15.6978 mL
    5 mM 0.3140 mL 1.5698 mL 3.1396 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, 1 year; -20°C, 6 months (sealed storage, away from moisture). When stored at -80°C, please use it within 1 year. When stored at -20°C, please use it within 6 months.

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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

    Concentration (start)

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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: 2.08 mg/mL (3.27 mM); Suspended solution; Need ultrasonic

      This protocol yields a suspended solution of 2.08 mg/mL. Suspended solution can be used for oral and intraperitoneal injection.

      Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (20.8 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% (20% SBE-β-CD in Saline)

      Solubility: ≥ 2.08 mg/mL (3.27 mM); Clear solution

      This protocol yields a clear solution of ≥ 2.08 mg/mL (saturation unknown).

      Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (20.8 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.

      Preparation of 20% SBE-β-CD in Saline (4°C, storage for one week): 2 g SBE-β-CD powder is dissolved in 10 mL Saline, completely dissolve until clear.

    For the following dissolution methods, please prepare the working solution directly. It is recommended to prepare fresh solutions and use them promptly within a short period of time.
    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:  20% HP-β-CD in Saline

      Solubility: 5 mg/mL (7.85 mM); Suspended solution; Need ultrasonic

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

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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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    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).

    *In solvent : -80°C, 1 year; -20°C, 6 months (sealed storage, away from moisture)

    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: 99.91%

    COA (243 KB) LCMS (99 KB)

    Handling Instructions (2659 KB)
    References
    Kinase Assay
    [1]

    To test compound inhibition against various RAF kinase isoforms, Sorafenib is added to a mixture of Raf-1 (80 ng), wt BRAF, or V599E BRAF (80 ng) with MEK-1 (1 μg) in assay buffer [20 mM Tris (pH 8.2), 100 mM NaCl, 5 mM MgCl2, and 0.15% β-mercaptoethanol] at a final concentration of 1% DMSO. The RAF kinase assay (final volume of 50 μL) is initiated by adding 25 μL of 10 μM γ-[33P]ATP (400 Ci/mol) and incubated at 32°C for 25 minutes. Phosphorylated MEK-1 is harvested by filtration onto a phosphocellulose mat, and 1% phosphoric acid is used to wash away unbound radioactivity. After drying by microwave heating, a β-plate counter is used to quantify filter-bound radioactivity[1].

    MCE has not independently confirmed the accuracy of these methods. They are for reference only.
    Cell Assay
    [2]

    The 10-0505, 06-0606, and 26-1004 tumors are finely minced and washed three times with modified Eagle medium (MEM). Cells are harvested by centrifuging at 800× g for 10 min. Cells are treated with 3 or 6 μM of Sorafenib in serum free MEM in the presence or absence of 5 μg/mL anti-human hepatocyte growth factor (HGF) antibody for 48 hrs. A total of 2 mL of conditioned medium from vehicle- or Sorafenib-treated (without anti-human antibody) is collected and concentrated using a VIVASPIN 20 and secreted HGF in conditioned medium is determined by western blotting[2].

    MCE has not independently confirmed the accuracy of these methods. They are for reference only.
    Animal Administration
    [2][3]

    Mice[2]
    For dose-response experiment, mice bearing the 06-0606 and 10-0505 xenografts are given four doses of Sorafenib (10, 30, 50 and 100 mg/kg daily) orally for 12 days. Each treatment group comprised of five mice. To investigate the antitumor effects of Sorafenib, mice bearing tumors are orally administered 50 mg/kg Sorafenib daily for 12 days. Each treatment group is comprised of 14 animals and each experiment is repeated at least twice. Treatment started on day 7 after tumor implantation. By this time, the HCC xenografts reached the size of approximately 100 mm3. To study the effects of Rapamycin plus Sorafenib on the growth of 10-0505 xenograft, mice bearing tumors (14 per group) are orally administered either 200 μL of vehicle, or 50 mg/kg of Sorafenib, or 1 mg/kg of Rapamycin, or Rapamycin plus Sorafenib daily for indicated days. Tumor growth is monitored at least twice weekly by Vernier caliper measurement of the length and width of tumor. Tumor volume is calculated as follows: [length×width2×π/6]. At the end of the study, the mice are killed with body and tumor weights being recorded, and the tumors harvested for analysis.
    Rats[3]
    In the study, 100- to 120-g male albino rats are utilized. After acclimatization period, rats are weighed and randomly divided into three groups: Group 1 (normal control group; n=10) is given the vehicle daily for 8 weeks. Group 2 (DENA group; n=15) receive i.p. single dose of 200 mg/kg DENA. Group 3 (Sorafenib group; n=12) is given Sorafenib orally at a dose of 10 mg/kg daily for 2 weeks, 6 weeks after DENA i.p. injection. At the end of the experiment (8 weeks), rats are weighed, anesthetized by ether, and killed, and their livers are dissected. Fresh liver is washed twice with ice-cold saline, dried on clean paper towel, and weighed. Liver index is calculated as liver weight (g)/final body weight (g)×100. The liver is divided into five portions: one portion is preserved in 10 % formalin for histopathological examination and the other portions are immediately frozen in liquid nitrogen and stored at −80°C.

    MCE has not independently confirmed the accuracy of these methods. They are for reference only.
    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, 1 year; -20°C, 6 months (sealed storage, away from moisture). When stored at -80°C, please use it within 1 year. When stored at -20°C, please use it within 6 months.

    Optional Solvent Concentration Solvent Mass 1 mg 5 mg 10 mg 25 mg
    DMSO 1 mM 1.5698 mL 7.8489 mL 15.6978 mL 39.2446 mL
    5 mM 0.3140 mL 1.5698 mL 3.1396 mL 7.8489 mL
    10 mM 0.1570 mL 0.7849 mL 1.5698 mL 3.9245 mL
    15 mM 0.1047 mL 0.5233 mL 1.0465 mL 2.6163 mL
    20 mM 0.0785 mL 0.3924 mL 0.7849 mL 1.9622 mL
    25 mM 0.0628 mL 0.3140 mL 0.6279 mL 1.5698 mL
    30 mM 0.0523 mL 0.2616 mL 0.5233 mL 1.3082 mL
    40 mM 0.0392 mL 0.1962 mL 0.3924 mL 0.9811 mL
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    Sorafenib Tosylate Related Classifications

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    • 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:

    Sorafenib475207-59-1Bay 43-9006RafVEGFRFLT3AutophagyFerroptosisApoptosisRaf kinasesVascular endothelial growth factor receptorCluster of differentiation antigen 135CD135Fms like tyrosine kinase 3Inhibitorinhibitorinhibit

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