Topotecan HCl
Topotecan HCl（SKF104864）is an inhibitor of topoisomerase 1 and semisynthetic analogue of camptothecin [1].
Topotecan HCl（SKF104864）has been reported to have a potent antitumor activity against tumors in murine models. In addition, Topotecan HCl has also shown the potent effect against intravenously implanted P388 leukemia and both intravenously and subcutaneously implanted Lewis lung carcinoma. Topotecan HCl has noted the activity against subcutaneously implanted solid tumors including chemorefractory tumors and human colon carcinoma xenograft HT-29. Topotecan HCl 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 HCl 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.
| Physical Appearance | A solid |
| Storage | Store at -20°C |
| M.Wt | 457.91 |
| Cas No. | 119413-54-6 |
| Formula | C23H24ClN3O5 |
| Solubility | ≥22.9 mg/mL in DMSO; insoluble in EtOH; ≥2.14 mg/mL in H2O with gentle warming and ultrasonic |
| 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 hydrochloride |
| SDF | Download SDF |
| Canonical SMILES | Cl[H].O=C1N(C([H])([H])C2=C([H])C(C(C([H])([H])N(C([H])([H])[H])C([H])([H])[H])=C3O[H])=C(C([H])=C3[H])N=C42)C4=C([H])C([C@@](C([H])([H])C([H])([H])[H])5O[H])=C1C([H])([H])OC5=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: | |
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Cell lines |
MCF-7 breast cancer cell line, human prostate cancer cell lines (PC-3 and LNCaP) |
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Preparation method |
The solubility of this compound in DMSO is >10 mM. General tips for obtaining a higher concentration: Please warm the tube at 37℃ for 10 minutes and/or shake it in the ultrasonic bath for a while. Stock solution can be stored below -20℃ for several months. |
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Reacting condition |
500 nM for 6-12 days; or 2, 10 nM for 72 h |
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Applications |
Topotecan-treated cells showed an impaired sphere-forming capacity in vitro. Topotecan-induced ABCG2 expression in MCF-7 cells was associated with decreased CD24/EpCAM expression [1]. Moreover, Topotecan treatment concentration-dependently increased the cytotoxicity in PC-3 and LNCaP cells [2]. |
| Animal experiment: | |
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Animal models |
Newborn NOD.Cg-Prkdcscid Il2rgtm1Wjl/SzJ (NSG) mice or adult NMRI-nu/nu mice model; PC-3 xenograft model |
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Dosage form |
2.45 and 0.10 mg/kg/day; intra-tumor injections, continuous infusion or conventional I.V., for 30 days; |
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Applications |
Topotecan-treated cells decreased tumorigenicity in immunodeficient mice [1]. Moreover, low-dose continuous administration of topotecan enhanced antitumor activity in prostate cancer [2]. |
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Other notes |
Please test the solubility of all compounds indoor, and the actual solubility may slightly differ with the theoretical value. This is caused by an experimental system error and it is normal. |
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References: 1. Huber, S., Wege, A. K., Bernhardt, G., Buschauer, A. and Brockhoff, G. (2015) Topotecan-induced ABCG2 expression in MCF-7 cells is associated with decreased CD24 and EpCAM expression and a loss of tumorigenicity. Cytometry A. 87, 707-716 2. Aljuffali, I. A., Mock, J. N., Costyn, L. J., Nguyen, H., Nagy, T., Cummings, B. S. and Arnold, R. D. (2011) Enhanced antitumor activity of low-dose continuous administration schedules of topotecan in prostate cancer. Cancer Biol Ther. 12, 407-420 | |
Quality Control & MSDS
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Chemical structure
