2. Cell Cycle/DNA Damage Autophagy Apoptosis
  3. Topoisomerase Autophagy Apoptosis
  4. Topotecan

Topotecan  (Synonyms: SKF 104864A; NSC 609669)

Cat. No.: HY-13768
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Topotecan (SKF 104864A; NSC 609669) is an orally active and potent Topoisomerase I inhibitor. Topotecan induces cell cycle arrest in G0/G1 and S phases and promotes apoptosis. Topotecan shows anticancer activity.

At equivalent molar concentrations, both the salt and free forms of a compound exhibit comparable biological activity. Nevertheless, the salt form (Topotecan hydrochloride) usually boasts enhanced water solubility and stability.

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

Topotecan Chemical Structure

Topotecan Chemical Structure

CAS No. : 123948-87-8

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Topotecan Related Antibodies

Top Publications Citing Use of Products

    Topotecan purchased from MedChemExpress. Usage Cited in: Nat Commun. 2019 Aug 21;10(1):3761.  [Abstract]

    IB analysis of the level of cleaved-caspase 3 and cleaved-PARP1 in the indicated chemotherapy-treated xenograft tumors. GAPDH served as the loading control.

    Topotecan purchased from MedChemExpress. Usage Cited in: Nat Commun. 2019 Aug 21;10(1):3761.  [Abstract]

    WDR5 inhibitor OICR-9429 enhances the sensitivity of ovarian cancer to genotoxic chemotherapeutics in vivo. Representative images and the apoptotic rate the indicated chemotherapy-treated xenograft tumors.

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    • Biological Activity

    • Protocol

    • Purity & Documentation

    • References

    • Customer Review

    Description

    Topotecan (SKF 104864A; NSC 609669) is an orally active and potent Topoisomerase I inhibitor. Topotecan induces cell cycle arrest in G0/G1 and S phases and promotes apoptosis. Topotecan shows anticancer activity[1].

    IC50 & Target[1]

    Topoisomerase I

     

    In Vitro

    Topotecan obviously inhibits proliferation of human glioma cells and glioma stem cells (GSCs) in a dose- and time-dependent manner[1].
    Topotecan (0-40 μM) obviously inhibits the cell viability compared with the control groups, in a dose-dependent manner[1].
    Topotecan shows anti-proliferation activity against U251, U87, GSCs-U251 and GSCs-U87 cells, with IC50 values of 2.73±0.25, 2.95±0.23, 5.46±0.41, and 5.95±0.24 μM, respectively[1].

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

    Topotecan Related Antibodies
    In Vivo

    NUB-7 metastatic model, the animals belonging to all the 4 groups are sacrificed after 14 days treatment. Compared with the control, Low dose metronomic (LDM) Topotecan (TP) and TP+Pazopanib (PZ) liver weights are significantly lower in TP+PZ-treated animals, compared with PZ. Microscopic tumors are visible in the livers of mice belonging to all the groups except TP+PZ confirming the ability of TP+PZ to control liver metastasis[2].
    Topotecan (0.5, 1.0, and 1.5 mg/kg; Orally, daily) causes greater reduction in microvascular density in an ovarian cancer model, but the mice treated with 1.5 mg/kg daily, oral Topotecan show decreased food intake, and a lesser antitumor effect[2].

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

    421.45

    Formula

    C23H23N3O5
    CAS No.
    SMILES

    O=C1[C@](O)(CC)C2=C(CO1)C(N3CC4=CC5=C(CN(C)C)C(O)=CC=C5N=C4C3=C2)=O
    Shipping

    Room temperature in continental US; may vary elsewhere.
    Storage

    Please store the product under the recommended conditions in the Certificate of Analysis.
    Solvent & Solubility
    In Vitro: 

    DMSO : 100 mg/mL (237.28 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 2.3728 mL 11.8638 mL 23.7276 mL
    5 mM 0.4746 mL 2.3728 mL 4.7455 mL
    View the Complete Stock Solution Preparation Table

    • 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

    Concentration (start)

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    Volume (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: 2.5 mg/mL (5.93 mM); Clear solution; Need ultrasonic

      This protocol yields a clear solution of 2.5 mg/mL.

      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% (20% SBE-β-CD in Saline)

      Solubility: 2.5 mg/mL (5.93 mM); Clear solution; Need ultrasonic

      This protocol yields a clear solution of 2.5 mg/mL.

      Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 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.
    In Vivo Dissolution Calculator
    Please enter the basic information of animal experiments:

    Dosage

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    Dosing volume
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    Number of animals

    Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
    Please enter your animal formula composition:
    %
    DMSO +
    % 
    +
    %
    Tween-80 +
    %
    Saline
    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
    References
    Cell Assay
    [1]

    The U251, U87, GSCs-U251 and GSCs-U87 cells are seeded at a density of 2×104 cells per well in 96-well plates separately, and incubated for 24 h. Cells are administered with Shikonin and Topotecan (0.02, 0.2, 2, 20, 40 μM). After the treatment, 10 μL of cell counting kit-8 (CCK-8) is added into each well for additional 1-hour incubation at 37°C. The optical density (OD) is read with a microplate reader at 450 nm[1].

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

    Mice[2]
    For subcutaneous xenograft studies, we used SK-N-BE, SH-SY5Y, KHOS, and RH30. 1×106 cells are implanted subcutaneously into the inguinal fat pad of each of nonobese diabetic/severe combined immune deficient (NOD/SCID) mice. When tumors reached 0.5 cm in diameter, the animals are randomized into 4 groups and treated daily by oral gavage. The animals are grouped as: Control group, LDM Topotecan group or LDM TP (1 mg/kg Topotecan), Pazopanib group or PZ (150 mg/kg Pazopanib) and combination group or TP+PZ (1 mg/kg Topotecan+150 mg/kg Pazopanib). To compare pulse Topotecan with LDM TP in KHOS osteosarcoma model, PZ is replaced by weekly oral dose of pulse Topotecan (SKF104864) or Pulse TP (15 mg/kg Topotecan (SKF104864)). The criteria for endpoint are tumor sizes exceeding 2.0 cm in diameter or animals showing signs of morbidity. The tumor sizes are measured on a daily basis until the endpoint or sacrifice. The long (D) and short diameters (d) are measured with calipers. Tumor volume (cm3) is calculated as V=0.5×D×d2. When the endpoint is reached or at the end of the treatment, the animals are sacrificed by cervical dislocation.

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

    Complete Stock Solution Preparation Table

    Optional Solvent Concentration Solvent Mass 1 mg 5 mg 10 mg 25 mg
    DMSO 1 mM 2.3728 mL 11.8638 mL 23.7276 mL 59.3190 mL
    5 mM 0.4746 mL 2.3728 mL 4.7455 mL 11.8638 mL
    10 mM 0.2373 mL 1.1864 mL 2.3728 mL 5.9319 mL
    15 mM 0.1582 mL 0.7909 mL 1.5818 mL 3.9546 mL
    20 mM 0.1186 mL 0.5932 mL 1.1864 mL 2.9660 mL
    25 mM 0.0949 mL 0.4746 mL 0.9491 mL 2.3728 mL
    30 mM 0.0791 mL 0.3955 mL 0.7909 mL 1.9773 mL
    40 mM 0.0593 mL 0.2966 mL 0.5932 mL 1.4830 mL
    50 mM 0.0475 mL 0.2373 mL 0.4746 mL 1.1864 mL
    60 mM 0.0395 mL 0.1977 mL 0.3955 mL 0.9887 mL
    80 mM 0.0297 mL 0.1483 mL 0.2966 mL 0.7415 mL
    100 mM 0.0237 mL 0.1186 mL 0.2373 mL 0.5932 mL
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    Topotecan 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:

    Topotecan123948-87-8SKF 104864A NSC 609669NSC609669NSC 609669NSC-609669TopoisomeraseAutophagyApoptosisU251U87GSCs-U251GSCs-U87orally activeInhibitorinhibitorinhibit

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