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

Topotecan hydrochloride  (Synonyms: SKF 104864A hydrochloride; NSC 609669 hydrochloride)

Cat. No.: HY-13768A Purity: 99.89%
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Topotecan Hydrochloride (SKF 104864A Hydrochloride) is a Topoisomerase I inhibitor with potent antineoplastic activities.

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

Topotecan hydrochloride Chemical Structure

Topotecan hydrochloride Chemical Structure

CAS No. : 119413-54-6

Size Price Stock Quantity
Solid + Solvent (Highly Recommended)
10 mM * 1 mL in DMSO
ready for reconstitution
 USD 66 In-stock
Solution
10 mM * 1 mL in DMSO USD 66 In-stock
Solid
5 mg USD 38 In-stock
10 mg USD 60 In-stock
50 mg USD 137 In-stock
100 mg USD 180 In-stock
200 mg   Get quote  
500 mg   Get quote  

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Customer Review

Based on 28 publication(s) in Google Scholar

Other Forms of Topotecan hydrochloride:

Topotecan hydrochloride Related Antibodies

Top Publications Citing Use of Products

    Topotecan hydrochloride 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.

    Topotecan hydrochloride 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.

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    Topoisomerase Topo I Topo II

    • Biological Activity

    • Protocol

    • Purity & Documentation

    • References

    • Customer Review

    Description

    Topotecan Hydrochloride (SKF 104864A Hydrochloride) is a Topoisomerase I inhibitor with potent antineoplastic activities.

    IC50 & Target[1]

    Topoisomerase I

     

    In Vitro

    Topotecan Hydrochloride (SKF 104864A Hydrochloride) obviously inhibits the proliferation of not only human glioma cells but also glioma stem cells (GSCs) in a dose- and time-dependent manner. According to the IC50 values at 24 h, 3 μM of Topotecan Hydrochloride is selected as the optimal administration concentration. In addition, Topotecan Hydrochloride induces cell cycle arrest in G0/G1 and S phases and promoted apoptosis. Results show that cell viability is inhibited by Topotecan Hydrochloride in a dose-dependent manner. 2, 20 and 40 μM of Topotecan Hydrochloride obviously inhibits the cell viability compared with the control groups. The IC50 values of Topotecan Hydrochloride at 24 h are 2.73±0.25 μM of U251 cells, 2.95±0.23 μM of U87 cells, 5.46±0.41 μM of GSCs-U251 and 5.95±0.24 μM of GSCs-U87. Thus 3 μM of Topotecan Hydrochloride is selected as the optimal administration concentration in the subsequent experiments[1].

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

    Topotecan hydrochloride Related Antibodies
    In Vivo

    NUB-7 metastatic model, the animals belonging to all the 4 groups are sacrificed after 14 days of treatment. Compared with the control, Low dose metronomic (LDM) Topotecan Hydrochloride 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 Topotecan Hydrochloride+PZ to control liver metastasis. In a previous dose-response study, the daily dose of oral metronomic Topotecan Hydrochloride (0.5, 1.0, and 1.5 mg/kg) causes greater reduction in microvascular density compared with weekly maximum-tolerated dose regimen (7.5 and 15 mg/kg) in an ovarian cancer model, but the mice treated with 1.5 mg/kg daily, oral Topotecan Hydrochloride 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

    457.91

    Formula

    C23H24ClN3O5
    CAS No.
    Appearance

    Solid

    Color

    Off-white to yellow

    SMILES

    [H]Cl.O=C1[C@](O)(CC)C2=C(CO1)C(N3CC4=CC5=C(CN(C)C)C(O)=CC=C5N=C4C3=C2)=O
    Structure Classification
    Initial Source
    Shipping

    Room temperature in continental US; may vary elsewhere.
    Storage

    4°C, sealed storage, away from moisture and light

    *In solvent : -80°C, 2 years; -20°C, 1 year (sealed storage, away from moisture and light)

    Solvent & Solubility
    In Vitro: 

    DMSO : 100 mg/mL (218.38 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

    H2O : 33.33 mg/mL (72.79 mM; Need ultrasonic)

    Preparing
    Stock Solutions
    Concentration Solvent Mass 1 mg 5 mg 10 mg
    1 mM 2.1838 mL 10.9192 mL 21.8384 mL
    5 mM 0.4368 mL 2.1838 mL 4.3677 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 (sealed storage, away from moisture and light). When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.

    * Note: If you choose water as the stock solution, please dilute it to the working solution, then filter and sterilize it with a 0.22 μm filter before use.

    • Molarity Calculator

    • Dilution Calculator

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

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    Molecular Weight *

    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    90% Corn Oil

      Solubility: ≥ 2.5 mg/mL (5.46 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.

    • Protocol 2

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

      Solubility: ≥ 2.08 mg/mL (4.54 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 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.
    In Vivo Dissolution Calculator
    Please enter the basic information of animal experiments:

    Dosage

    mg/kg

    Animal weight
    (per animal)

    g

    Dosing volume
    (per animal)

    μL

    Number of animals

    Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
    Calculation results:
    Working solution concentration: mg/mL
    This product has good water solubility, please refer to the measured solubility data in water/PBS/Saline for details.
    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).
    Purity & Documentation

    Purity: 99.89%

    COA (256 KB) LCMS (94 KB)

    Handling Instructions (2659 KB)
    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 Hydrochloride (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 Hydrochloride + 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 or Pulse TP (15 mg/kg Topotecan). 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

    * 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 (sealed storage, away from moisture and light). 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
    H2O / DMSO 1 mM 2.1838 mL 10.9192 mL 21.8384 mL 54.5959 mL
    5 mM 0.4368 mL 2.1838 mL 4.3677 mL 10.9192 mL
    10 mM 0.2184 mL 1.0919 mL 2.1838 mL 5.4596 mL
    15 mM 0.1456 mL 0.7279 mL 1.4559 mL 3.6397 mL
    20 mM 0.1092 mL 0.5460 mL 1.0919 mL 2.7298 mL
    25 mM 0.0874 mL 0.4368 mL 0.8735 mL 2.1838 mL
    30 mM 0.0728 mL 0.3640 mL 0.7279 mL 1.8199 mL
    40 mM 0.0546 mL 0.2730 mL 0.5460 mL 1.3649 mL
    50 mM 0.0437 mL 0.2184 mL 0.4368 mL 1.0919 mL
    60 mM 0.0364 mL 0.1820 mL 0.3640 mL 0.9099 mL
    DMSO 80 mM 0.0273 mL 0.1365 mL 0.2730 mL 0.6824 mL
    100 mM 0.0218 mL 0.1092 mL 0.2184 mL 0.5460 mL

    * Note: If you choose water as the stock solution, please dilute it to the working solution, then filter and sterilize it with a 0.22 μm filter before use.

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    Topotecan hydrochloride 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:

    Topotecan119413-54-6SKF 104864ANSC 609669NSC609669NSC-609669TopoisomeraseAutophagyApoptosisInhibitorinhibitorinhibit

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