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Submit ReviewTopotecan hydrochloride
Description: DNA topoisomerase I inhibitor; Camptothecin (Cat. No. 1100) analog
Alternative Names: SK&F 104864-A
Chemical Name: 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
Purity: ≥98% (HPLC)
Biological Activity for Topotecan hydrochloride
Topotecan hydrochloride is a DNA topoisomerase I inhibitor; induces rapid apoptotic death in human B-lineage acute lymphoblastic leukemia (ALL) cells. Improves survival in three mouse models of poor prognosis ALL; downregulates B-Myb and MycN expression in neuroblastoma cells. Water-soluble analog of Camptothecin (Cat. No. 1100). Orally bioavailable. Topotecan disrupts the interaction between NHP2L1 and U4 RNA by binding to U4 and inhibits RNA splicing.
Technical Data for Topotecan hydrochloride
| M. Wt | 457.91 |
| Formula | C23H23N3O5.HCl |
| Storage | Store at -20°C |
| Purity | ≥98% (HPLC) |
| CAS Number | 119413-54-6 |
| PubChem ID | 60699 |
| InChI Key | DGHHQBMTXTWTJV-BQAIUKQQSA-N |
| Smiles | OC1=CC=C(N=C(C(N3C4)=CC([C@](CC)(O)C(OC5)=O)=C5C3=O)C4=C2)C2=C1CN(C)C.Cl |
The technical data provided above is for guidance only. For batch specific data refer to the Certificate of Analysis.
Tocris products are intended for laboratory research use only, unless stated otherwise.
Solubility Data for Topotecan hydrochloride
| Solvent | Max Conc. mg/mL | Max Conc. mM | |
|---|---|---|---|
| Solubility | |||
| water | 45.79 | 100 | |
| DMSO | 45.79 | 100 |
Preparing Stock Solutions for Topotecan hydrochloride
The following data is based on the product molecular weight 457.91. Batch specific molecular weights may vary from batch to batch due to the degree of hydration, which will affect the solvent volumes required to prepare stock solutions.
| Concentration / Solvent Volume / Mass | 1 mg | 5 mg | 10 mg |
|---|---|---|---|
| 1 mM | 2.18 mL | 10.92 mL | 21.84 mL |
| 5 mM | 0.44 mL | 2.18 mL | 4.37 mL |
| 10 mM | 0.22 mL | 1.09 mL | 2.18 mL |
| 50 mM | 0.04 mL | 0.22 mL | 0.44 mL |
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Product Datasheets for Topotecan hydrochloride
References for Topotecan hydrochloride
References are publications that support the biological activity of the product.
Uckun et al (1995) In vitro and in vivo activity of topo. against human B-lineage acute lymphoblastic leukemia cells. Blood 85 2817 PMID: 7742543
Sottile et al (2012) A chemical screen identifies the chemotherapeutic drug topo. as a specific inhibitor of the B-MYB/MYCN axis in neuroblastoma. Oncotarget. 3 535 PMID: 22619121
Schellens et al (1996) Bioavailability and pharmacokinetics of oral topotecan: a new topoisomerase I inhibitor. Br.J.Cancer 73 1268 PMID: 8630291
If you know of a relevant reference for Topotecan hydrochloride, please let us know.
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6 Citations for Topotecan hydrochloride
Citations are publications that use Tocris products. Selected citations for Topotecan hydrochloride include:
Florea et al (2017) Calcium-regulatory proteins as modulators of chemotherapy in human neuroblastoma. Oncotarget 8 22876 PMID: 28206967
Michael G et al (2021) Loss of Aurora Kinase Signaling Allows Lung Cancer Cells to Adopt Endoreplication and Form Polyploid Giant Cancer Cells That Resist Antimitotic Drugs. Cancer Res 81 400-413 PMID: 33172929
Balmus et al (2019) ATM orchestrates the DNA-damage response to counter toxic non-homologous end-joining at broken replication forks. Nat Commun 10 87 PMID: 30622252
Martin et al (2017) Molecular Phenotyping Combines Molecular Information, Biological Relevance, and Patient Data to Improve Productivity of Early Drug Discovery. Cell Chem Biol 24 624-634.e3 PMID: 28434878
Pearson et al (2016) Identification of chemicals that mimic transcriptional changes associated with autism, brain aging and neurodegeneration. Int J Mol Med 7 11173 PMID: 27029645
Jen Q et al (2022) Ion Channel Drugs Suppress Cancer Phenotype in NG108-15 and U87 Cells: Toward Novel Electroceuticals for Glioblastoma. Cancers (Basel) 14 PMID: 35326650
Do you know of a great paper that uses Topotecan hydrochloride from Tocris? Please let us know.
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Literature in this Area
Tocris offers the following scientific literature in this area to showcase our products. We invite you to request* your copy today!
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Huntington's Disease Research Product Guide
This product guide provides a background to Huntington's disease research and lists around 100 products for the study of:
- Somatic Instability
- Proteolysis and Inclusion Bodies
- Transcriptional Dysregulation
- Mitochondrial Dysfunction
- Nuclear-Cytoplasmic Transport Interference
- Excitotoxicity
- Stem Cells
Cell Cycle & DNA Damage Repair Poster
In normal cells, each stage of the cell cycle is tightly regulated, however in cancer cells many genes and proteins that are involved in the regulation of the cell cycle are mutated or over expressed. This poster summarizes the stages of the cell cycle and DNA repair. It also highlights strategies for enhancing replicative stress in cancer cells to force mitotic catastrophe and cell death.