Biological Activity
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.
Technical Data
| 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.
All Tocris products are intended for laboratory research use only.
Solubility Data
| Solvent | Max Conc. mg/mL | Max Conc. mM | |
|---|---|---|---|
| Solubility | |||
| DMSO | 45.79 | 100 | |
| water | 45.79 | 100 |
Preparing Stock Solutions
The following data is based on the product molecular weight 457.91. Batch specific molecular weights may vary from batch to batch due to solvent 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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References
References are publications that support the products' biological activity.
Uckun et al (1995) In vitro and in vivo activity of topotecan against human B-lineage acute lymphoblastic leukemia cells. Blood 85 2817 PMID: 7742543
Sottile et al (2012) A chemical screen identifies the chemotherapeutic drug topotecan 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
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