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

Sorafenib Tosylate (Synonyms: Bay 43-9006 (Tosylate))

Cat. No.: HY-10201A Purity: 99.53%
Handling Instructions

Sorafenib tosylate is a potent multikinase inhibitor, with IC50s of 6 nM, 20 nM, and 22 nM for Raf-1, B-Raf, and VEGFR-3, respectively.

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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10 mM * 1 mL in DMSO USD 66 In-stock
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Estimated Time of Arrival: December 31
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Estimated Time of Arrival: December 31
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Customer Review

Other Forms of Sorafenib Tosylate:

Top Publications Citing Use of Products

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

    Valproic acid (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 MCE. Usage Cited in: Br J Cancer. 2017 Sep 26;117(7):974-983.

    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 MCE. Usage Cited in: Int J Clin Exp Pathol. 2015 Apr 1;8(4):3871-81.

    The relationship between SOX9 and Raf/MEK/ERK signaling pathway. Co-treatment of si-SOX9-1 and Sorafenib (10uM, 15uM)/Sunitinib (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).

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

    The relationship between SOX9 and Raf/MEK/ERK signaling pathway. Co-treatment of si-SOX9-1 and Sorafenib (10uM, 15uM)/Sunitinib (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 MCE. Usage Cited in: Oncotarget. 2017 May 2;8(18):29771-29784.

    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 MCE. Usage Cited in: J Pharmacol Exp Ther. 2017 Aug;362(2):219-229.

    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 MCE. Usage Cited in: Endocr J. 2017 Nov 29;64(11):1115-1123.

    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 MCE. Usage Cited in: Endocr J. 2017 Nov 29;64(11):1115-1123.

    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 MCE. Usage Cited in: Int J Biol Sci. 2018 Apr 25;14(5):577-585.

    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 MCE. Usage Cited in: Oncol Rep. 2018 Sep;40(3):1525-1532.

    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.

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    • Biological Activity

    • Protocol

    • Technical Information

    • Purity & Documentation

    • References

    Description

    Sorafenib tosylate is a potent multikinase inhibitor, with IC50s of 6 nM, 20 nM, and 22 nM for Raf-1, B-Raf, and VEGFR-3, respectively.

    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-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].

    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].

    Clinical Trial
    Storage
    Powder -20°C 3 years
      4°C 2 years
    In solvent -80°C 6 months
      -20°C 1 month
    Solvent & Solubility
    In Vitro: 

    DMSO : ≥ 31 mg/mL (48.66 mM)

    H2O : < 0.1 mg/mL (insoluble)

    *"≥" 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
    10 mM 0.1570 mL 0.7849 mL 1.5698 mL
    *Please refer to the solubility information to select the appropriate solvent.
    In Vivo:
    • 1.

      Sorafenib tosylate is dissolved in solvent (cremophor EL/ethanol, 50%:50%)[4].

    *All of the co-solvents are provided by MCE.
    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
    Molecular Weight

    637.03

    Formula

    C₂₈H₂₄ClF₃N₄O₆S

    CAS No.

    475207-59-1

    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

    Purity: 99.53%

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    Product Name:
    Sorafenib Tosylate
    Cat. No.:
    HY-10201A
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    Sorafenib Tosylate

    Cat. No.: HY-10201A