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Purity: ≥98%
Topotecan HCl (formerly known as NSC609699, Nogitecan, NSC-609699, SKFS-104864A; trade name: Hycamtin), an FDA approved drug for cancer treatment, is a topoisomerase I inhibitor with potent antineoplastic activity. In cell-free assays, it inhibits topoisomerase I in MCF-7 Luc and DU-145 Luc cells with IC50 values of 13 nM and 2 nM, respectively. A semisynthetic derivative of camptothecin with antitumor properties is topotecan. Topotecan selectively stabilizes topoisomerase I-DNA covalent complexes during the S phase of the cell cycle. This prevents topoisomerase I-mediated single-strand DNA breaks from religating and creates potentially fatal double-strand DNA breaks when the DNA replication machinery comes into contact with the complexes.
Targets |
Topo I (DU-145 Luc cells) ( IC50 = 2 nM ); Topo I (MCF-7 Luc cells) ( IC50 = 13 nM )
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ln Vitro |
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ln Vivo |
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Cell Assay |
Topotecan is first diluted to 6 μg/mL in cultured medium after being dissolved in sterile water to a stock concentration of 1 mg/mL. The final volume of each opaque, white tissue culture-treated microplate is achieved by serially diluting the solution 1:4 until it is 0.1 mL/well. 100 μL of cells are added to each well. MCF-7 Luc and DU-145 Luc cells are resuspended in 3×104 cells/mL in DMEM with high glucose containing 10% FBS and 0.5 mg/mL Geneticin. Plates are incubated for four days at 37 °C with 5% CO2 and 95% humidity. Each well receives 0.05 mL of 0.1 M HEPES buffer (pH 7.9) containing 50 μg/mL D-luciferin after incubation. The culture microplate is measured in a molecular light imager and a microplate luminometer after being incubated at room temperature for ten minutes. The microplate luminometer's results are computed using maximum inhibition control wells that contain an ATP inhibitor and no inhibition control wells that do not contain an exogenous drug. The values acquired with a 5-minute luminescent imager are used in a similar manner to calculate the results for the molecular light imager.
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Animal Protocol |
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References |
Molecular Formula |
C23H23N3O5.HCL
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Molecular Weight |
457.91
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Exact Mass |
457.14
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Elemental Analysis |
C, 60.33; H, 5.28; Cl, 7.74; N, 9.18; O, 17.47
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CAS # |
119413-54-6
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Appearance |
Yellow solid powder
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SMILES |
CC[C@@]1(C2=C(COC1=O)C(=O)N3CC4=CC5=C(C=CC(=C5CN(C)C)O)N=C4C3=C2)O.Cl
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InChi Key |
DGHHQBMTXTWTJV-BQAIUKQQSA-N
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InChi Code |
InChI=1S/C23H23N3O5.ClH/c1-4-23(30)16-8-18-20-12(9-26(18)21(28)15(16)11-31-22(23)29)7-13-14(10-25(2)3)19(27)6-5-17(13)24-20;/h5-8,27,30H,4,9-11H2,1-3H3;1H/t23-;/m0./s1
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Chemical Name |
(19S)-8-[(dimethylamino)methyl]-19-ethyl-7,19-dihydroxy-17-oxa-3,13-diazapentacyclo[11.8.0.02,11.04,9.015,20]henicosa-1(21),2,4(9),5,7,10,15(20)-heptaene-14,18-dione;hydrochloride
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Synonyms |
NSC609699; SKF-104864-A; NSC 609699; SKF 104864 A; NSC-609699; SKF S104864A; Nogitecan HCl; SKFS 104864A; SKF104864A; TOPO. Hycamtamine; Hycamtin Hydrochloride; Nogitecan Hydrochloride; Topotecan; Nogitecan Hydrochloride; Trade name: Hycamtin
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HS Tariff Code |
2934.99.9001
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Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month |
Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
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Solubility (In Vitro) |
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Solubility (In Vivo) |
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Preparing Stock Solutions | 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 | |
10 mM | 0.2184 mL | 1.0919 mL | 2.1838 mL |
*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.
Calculation results
Working concentration: mg/mL;
Method for preparing DMSO stock solution: mg drug pre-dissolved in μL DMSO (stock solution concentration mg/mL). Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug.
Method for preparing in vivo formulation::Take μL DMSO stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O,mix and clarify.
(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
(2) Be sure to add the solvent(s) in order.
NCT Number | Recruitment | interventions | Conditions | Sponsor/Collaborators | Start Date | Phases |
NCT02030964 | Active Recruiting |
Drug: Topotecan Drug: DFMO |
Neuroblastoma | New Approaches to Neuroblastoma Therapy Consortium |
December 2013 | Phase 1 |
NCT02298348 | Active Recruiting |
Drug: Topotecan Drug: Sorafenib |
Neuroblastoma | New Approaches to Neuroblastoma Therapy Consortium |
April 2015 | Phase 1 |
NCT03600649 | Active Recruiting |
Drug: Topotecan Drug: Seclidemstat |
Ewing Sarcoma Myoepithelial Tumor |
Salarius Pharmaceuticals, LLC | June 4, 2018 | Phase 1 |
NCT02487095 | Active Recruiting |
Drug: Topotecan Drug: VX-970 (M6620) |
Small Cell Lung Carcinoma Ovarian Neoplasms |
National Cancer Institute (NCI) |
July 30, 2015 | Phase 1 Phase 2 |
NCT00638898 | Active Recruiting |
Drug: topotecan hydrochloride Drug: busulfan |
Solid Tumor Ewing Sarcoma |
City of Hope Medical Center | February 26, 2007 | Phase 1 |
Internucleosomal DNA fragmentation in topotecan-treated B-lineage ALL cells. Blood . 1995 May 15;85(10):2817-28. td> |
(A and B) Ultrastructural features of topotecan treated ALL cells undergoing apoptosis. Blood . 1995 May 15;85(10):2817-28. td> |
Nanomolar concentrations of topotecan induce apoptotic cell death of radiation-resistant RS4;11 leukemia cells expressing high levels of bcl-2 protein. Blood . 1995 May 15;85(10):2817-28. td> |