Topotecan
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.
- 1. Lambo S, Gr?bner SN, et al. "The molecular landscape of ETMR at diagnosis and relapse." Nature. 2019 Dec;576(7786):274-280. PMID:31802000
- 2. Manasi Ratnaparkhe, John Wong, et al. "Defective DNA damage repair leads to frequent catastrophic genomic events in murine and human tumors." bioRxiv. 2018 May 4.
| Physical Appearance | A solid |
| Storage | Store at -20°C |
| M.Wt | 421.45 |
| Cas No. | 123948-87-8 |
| Formula | C23H23N3O5 |
| Solubility | ≥21.1 mg/mL in DMSO; insoluble in EtOH; insoluble in H2O |
| 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 |
| SDF | Download SDF |
| Canonical SMILES | CC[C@]1(O)C(C=C2C3=NC4=CC=C(O)C(CN(C)C)=C4C=C3CN2C5=O)=C5COC1=O |
| Shipping Condition | Small Molecules with Blue Ice, Modified Nucleotides with Dry Ice. |
| General tips | We do not recommend long-term storage for the solution, please use it up soon. |
| Cell experiment:[1] | |
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Cell lines |
Human glioma cell lines U251, U87, GSCs-U251 and GSCs-U87 |
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Reaction Conditions |
0.02, 0.2, 2, 20 or 40 μmol/L topotecan for 12, 24 or 48 h incubation |
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Applications |
Topotecan obviously inhibited proliferation of not only human glioma cells but also glioma stem cells in a dose- and time-dependent manner. In addition, topotecan (3 μmol/L, 24 h) induced cell cycle arrest in G0/G1 and S phases and promoted apoptosis. |
| Animal experiment:[2] | |
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Animal models |
Mouse models of aggressive pediatric solid tumor |
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Dosage form |
1 mg/kg Once daily by oral gavage |
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Applications |
Metronomic administration of topotecan and pazopanib showed a statistically significant antitumor activity compared with respective single agents in pediatric tumor mouse models, representing a valid option as a maintenance therapy in aggressive pediatric solid tumors. |
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Note |
The technical data provided above is for reference only. |
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References: 1. Zhang FL, Wang P, Liu YH, et al. Topoisomerase I inhibitors, shikonin and topotecan, inhibit growth and induce apoptosis of glioma cells and glioma stem cells. PLoS One, 2013, 8(11): e81815. 2. Kumar S, Mokhtari RB, Sheikh R, et al. Metronomic oral topotecan with pazopanib is an active antiangiogenic regimen in mouse models of aggressive pediatric solid tumor. Clinical Cancer Research, 2011, 17(17): 5656-5667. |
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Quality Control & MSDS
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Chemical structure
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