2. Protein Tyrosine Kinase/RTK Metabolic Enzyme/Protease Stem Cell/Wnt JAK/STAT Signaling Apoptosis
  3. SHP1 Phosphatase STAT Apoptosis
  4. SC-43

SC-43, a Sorafenib derivative, is a potent and orally active SHP-1 (PTPN6) agonist. SC-43 inhibits the phosphorylation of STAT3 and induces cell apoptosis. SC-43 has anti-fibrotic and anticancer effects.

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

CAS No. : 1400989-25-4

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Solid + Solvent (Highly Recommended)
10 mM * 1 mL in DMSO
ready for reconstitution
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Customer Review

Based on 6 publication(s) in Google Scholar

SC-43 Related Antibodies

Top Publications Citing Use of Products

    SC-43 purchased from MedChemExpress. Usage Cited in: J Clin Invest. 2024 Oct 1;134(24):e183161.  [Abstract]

    SC-43 (10 mg/kg; oral gavage; three intermittent doses before and after LPS administration) treatment reduced alveolar neutrophils and CitH3-DNA NET complexes, while alveolar protein leakage and NE-DNA NET levels were unchanged..

    SC-43 purchased from MedChemExpress. Usage Cited in: J Clin Invest. 2024 Oct 1;134(24):e183161.  [Abstract]

    Lung H&E stained tissue in DMSO control and SC43 (SC-43) (10 mg/kg; oral gavage; three intermittent doses before and after LPS administration) treated mice indicating reduced perihilar inflammation with SC43 administration.

    SC-43 purchased from MedChemExpress. Usage Cited in: J Clin Invest. 2024 Oct 1;134(24):e183161.  [Abstract]

    Dose-dependent reduction in LPS-induced ROS (superoxide release) production with SC43 (SC-43) (10 mg/kg; oral gavage; three intermittent doses before and after LPS administration) versus DMSO (vehicle) control (n = 3).

    SC-43 purchased from MedChemExpress. Usage Cited in: J Pharm Biomed Anal. 2024 May 15:242:116023.  [Abstract]

    Effect of SC-43 with various concentrations on the cell viability at various time points. Cells were treated with SC-43 (0.78-100 μM) at various concentrations for 2 h、4 h、8 h、12 h and 24 h. Cell viability was determined by the Cell Counting Kit-8.

    SC-43 purchased from MedChemExpress. Usage Cited in: J Pharm Biomed Anal. 2024 May 15:242:116023.  [Abstract]

    Effect of SC-43 with different concentrations on the RPA1 and TAP1 protein levels in HepG2 cells. Cells were treated with SC-43 (3.125-25 μM) at various concentrations for 2 h. The protein level was determined by the ELISA kit.

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    • Biological Activity

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    Description

    SC-43, a Sorafenib derivative, is a potent and orally active SHP-1 (PTPN6) agonist. SC-43 inhibits the phosphorylation of STAT3 and induces cell apoptosis. SC-43 has anti-fibrotic and anticancer effects[1][2].

    IC50 & Target[1][2]

    SHP-1

     

    p-STAT3

     

    In Vitro

    SC-43 (0-10 μM; 24-72 hours; HuCCT-1, KKU-100, and CGCCA cells) treatment reveals the anti-proliferative effects in cholangiocarcinoma (CCA) cell lines in a dose-dependent manner after treating 24, 48 and 72 hours respectively[1].
    SC-43 (0-10 μM; 24 hours; HuCCT-1, KKU-100, and CGCCA cells) treatment shows increased sub-G1 cells and G2-M arrest, indicating SC-43 induced differential apoptotic effects in these cell lines[1].
    SC-43 (0-10 μM; 24 hours; HuCCT-1, KKU-100, and CGCCA cells) treatment demonstrates significant increase in cleaved caspase-3 and PARP level[1].
    SC-43 activates SH2 domain-containing phosphatase 1 (SHP-1) activity, leading to p-STAT3 and downstream cyclin B1 and Cdc2 downregulation. SC-43 augments SHP-1 activity by direct binding to N-SH2 and relief of its autoinhibition[1].

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

    SC-43 Related Antibodies

    Cell Viability Assay[1]

    Cell Line: HuCCT-1, KKU-100, and CGCCA cells
    Concentration: 0 μM, 0.25 μM, 0.5 μM, 0.75 μM, 1 μM, 2.5 μM, 5 μM, 10 μM
    Incubation Time: 24 hours, 48 hours, 72 hours
    Result: Revealed the anti-proliferative effects in CCA cell lines in a dose-dependent manner after treating 24, 48 and 72 hours respectively.

    Cell Cycle Analysis[1]

    Cell Line: HuCCT-1, KKU-100, and CGCCA cells
    Concentration: 0 μM, 1 μM, 2.5 μM, 5 μM, 10 μM
    Incubation Time: 24 hours
    Result: Showed increased sub-G1 cells and G2-M arrest.

    Western Blot Analysis[1]

    Cell Line: HuCCT-1, KKU-100, and CGCCA cells
    Concentration: 0 μM, 1 μM, 2.5 μM, 5 μM, 10 μM
    Incubation Time: 24 hours
    Result: Demonstrated significant increase in cleaved caspase-3 and PARP level.
    In Vivo

    SC-43 (10-30 mg/kg; oral gavage; daily; for 23 days; male NCr athymic nude mice) treatment exhibits xenograft tumor growth inhibition, p-STAT3 reduction and SHP-1 activity elevation[1].

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

    Animal Model: Male NCr athymic nude mice (5-7 weeks of age) injected with HuCCT-1 cells[1]
    Dosage: 10 mg/kg or 30 mg/kg
    Administration: Oral gavage; daily; for 23 days
    Result: Exhibited xenograft tumor growth inhibition, p-STAT3 reduction and SHP-1 activity elevation.
    Clinical Trial
    Molecular Weight

    431.80

    Formula

    C21H13ClF3N3O2
    CAS No.
    Appearance

    Solid

    Color

    White to off-white

    SMILES

    O=C(NC1=CC=CC(OC2=CC=C(C#N)C=C2)=C1)NC3=CC=C(Cl)C(C(F)(F)F)=C3
    Shipping

    Room temperature in continental US; may vary elsewhere.
    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 : 250 mg/mL (578.97 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 2.3159 mL 11.5794 mL 23.1589 mL
    5 mM 0.4632 mL 2.3159 mL 4.6318 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, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

    • Molarity Calculator

    • Dilution Calculator

    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: 2.08 mg/mL (4.82 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% Corn Oil

      Solubility: ≥ 2.08 mg/mL (4.82 mM); Clear solution

      This protocol yields a clear solution of ≥ 2.08 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 (20.8 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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    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: 99.01%

    SDS (393 KB)

    COA (244 KB) HNMR (266 KB) LCMS (97 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, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

    Optional Solvent Concentration Solvent Mass 1 mg 5 mg 10 mg 25 mg
    DMSO 1 mM 2.3159 mL 11.5794 mL 23.1589 mL 57.8972 mL
    5 mM 0.4632 mL 2.3159 mL 4.6318 mL 11.5794 mL
    10 mM 0.2316 mL 1.1579 mL 2.3159 mL 5.7897 mL
    15 mM 0.1544 mL 0.7720 mL 1.5439 mL 3.8598 mL
    20 mM 0.1158 mL 0.5790 mL 1.1579 mL 2.8949 mL
    25 mM 0.0926 mL 0.4632 mL 0.9264 mL 2.3159 mL
    30 mM 0.0772 mL 0.3860 mL 0.7720 mL 1.9299 mL
    40 mM 0.0579 mL 0.2895 mL 0.5790 mL 1.4474 mL
    50 mM 0.0463 mL 0.2316 mL 0.4632 mL 1.1579 mL
    60 mM 0.0386 mL 0.1930 mL 0.3860 mL 0.9650 mL
    80 mM 0.0289 mL 0.1447 mL 0.2895 mL 0.7237 mL
    100 mM 0.0232 mL 0.1158 mL 0.2316 mL 0.5790 mL
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    SC-43 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:

    SC-431400989-25-4SC43SC 43SHP1PhosphataseSTATApoptosisShp1PTPN6Src homology region 2 (SH-2) domain-containing phosphatase 1SHP-1antiproliferativep-STAT3anti-fibroticanticancerorallycaspase-3PARPInhibitorinhibitorinhibit

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