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Topotecan

Catalog No.GC17833

Topoisomerase 1 inhibitor

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Topotecan Chemical Structure

Cas No.: 123948-87-8

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10mM (in 1mL DMSO)
$36.00
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10mg
$29.00
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50mg
$99.00
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100mg
$104.00
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Sample solution is provided at 25 µL, 10mM.

Product Documents

Quality Control & SDS

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Protocol

Cell experiment:

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].

Animal experiment:

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.

References:

[1]. Zhang FL, et al. PLoS One. 2013 Nov 26;8(11):e81815.Topoisomerase I inhibitors, Shikonin and Topotecan, inhibit growth and induce apoptosis of glioma cells andglioma stem cells.
[2]. Kumar S, et al. Metronomic oral topotecan with pazopanib is an active antiangiogenic regimen in mouse models of aggressive pediatric solid tumor. Clin Cancer Res. 2011 Sep 1;17(17):5656-67.

Background

Topotecan (SKF104864) is an inhibitor of topoisomerase 1 and semisynthetic analogue of camptothecin [1].

Topotecan (SKF104864) has been reported to have a potent antitumor activity against tumors in murine models. In addition, Topotecan has also shown the potent effect against intravenously implanted P388 leukemia and both intravenously and subcutaneously implanted Lewis lung carcinoma. Topotecan has noted the activity against subcutaneously implanted solid tumors including chemorefractory tumors and human colon carcinoma xenograft HT-29. Topotecan has been found to induce regressions in the lung tumor model (Lewis lung carcinoma and B16 melanoma), compared to camptothecin and 9-amino-camptothecin. In the preclinical toxicology studies, Topotecan has been revealed to have a concentration-dependent, reversible and limited toxoicity to rapidly proliferation tissues such as bone marrow and gastro-intestinal epithelium [1].

References:
[1] Creemers GJ1, Lund B, Verweij J. Topoisomerase I inhibitors: topotecan and irenotecan. Cancer Treat Rev. 1994 Jan;20(1):73-96.

Chemical Properties

Cas No. 123948-87-8 SDF
Chemical Name (S)-10-((dimethylamino)methyl)-4-ethyl-4,9-dihydroxy-1H-pyrano[3',4':6,7]indolizino[1,2-b]quinoline-3,14(4H,12H)-dione
Canonical SMILES CC[C@]1(O)C(C=C2C3=NC4=CC=C(O)C(CN(C)C)=C4C=C3CN2C5=O)=C5COC1=O
Formula C23H23N3O5 M.Wt 421.45
Solubility ≥ 21.1mg/mL in DMSO Storage Store at -20°C,protect from light
General tips Please select the appropriate solvent to prepare the stock solution according to the solubility of the product in different solvents; once the solution is prepared, please store it in separate packages to avoid product failure caused by repeated freezing and thawing.Storage method and period of the stock solution: When stored at -80°C, please use it within 6 months; when stored at -20°C, please use it within 1 month.
To increase solubility, heat the tube to 37°C and then oscillate in an ultrasonic bath for some time.
Shipping Condition Evaluation sample solution: shipped with blue ice. All other sizes available: with RT, or with Blue Ice upon request.

Complete Stock Solution Preparation Table

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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
10 mM 0.2373 mL 1.1864 mL 2.3728 mL
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Average Rating: 5 ★★★★★ (Based on Reviews and 32 reference(s) in Google Scholar.)

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