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Submit ReviewMitoxantrone dihydrochloride
Description: Topoisomerase II inhibitor; immunosuppressive and antineoplastic agent
Chemical Name: 1,4-Dihydroxy-5,8-bis[[2-[(2-hydroxyethyl)amino]ethyl]amino]-9,10-anthracenedione dihydrochloride
Purity: ≥98% (HPLC)
Biological Activity for Mitoxantrone dihydrochloride
Mitoxantrone dihydrochloride is a type II DNA topoisomerase inhibitor. Disrupts DNA synthesis and repair and induces damage by DNA cross-linking. Also inhibits PIM1 kinase (IC50 = 51 nM). Immunomodulatory, antineoplastic and chemotherapeutic agent. Also USP11 inhibitor (IC50= 3.15 μM). Induces cell death of pancreatic cancer cell lines expressing wild-type BRCA2.
Technical Data for Mitoxantrone dihydrochloride
| M. Wt | 517.4 |
| Formula | C22H28N4O6.2HCl |
| Storage | Desiccate at RT |
| Purity | ≥98% (HPLC) |
| CAS Number | 70476-82-3 |
| PubChem ID | 51082 |
| InChI Key | ZAHQPTJLOCWVPG-UHFFFAOYSA-N |
| Smiles | O=C2C3=C(C(O)=CC=C3O)C(C1=C(NCCNCCO)C=CC(NCCNCCO)=C12)=O.Cl.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 Mitoxantrone dihydrochloride
| Solvent | Max Conc. mg/mL | Max Conc. mM | |
|---|---|---|---|
| Solubility | |||
| water | 2.59 | 5 | |
| DMSO | 38.8 | 75 |
Preparing Stock Solutions for Mitoxantrone dihydrochloride
The following data is based on the product molecular weight 517.4. 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 |
|---|---|---|---|
| 0.75 mM | 2.58 mL | 12.88 mL | 25.77 mL |
| 3.75 mM | 0.52 mL | 2.58 mL | 5.15 mL |
| 7.5 mM | 0.26 mL | 1.29 mL | 2.58 mL |
| 37.5 mM | 0.05 mL | 0.26 mL | 0.52 mL |
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Product Datasheets for Mitoxantrone dihydrochloride
References for Mitoxantrone dihydrochloride
References are publications that support the biological activity of the product.
Scott and Figgit (2004) Mitoxantrone: a review of its uses in multiple sclerosis. CNS Drugs. 18 379 PMID: 15089110
Crespi et al (1986) Mitoxantrone affects topoisomerase activities in human breast cancer cells. Biochem.Biophys.Res.Comm. 136 521 PMID: 3010982
Wan et al (2013) A new target for an old drug: identifying mitoxan. as a nanomolar inhibitor of PIM1 kinase via kinome-wide selectivity modeling. J.Med.Chem. 56 2619 PMID: 23442188
Burkhart et al (2013) Mitoxantrone targets human ubiquitin-specific peptidase 11 (USP11) and is a potent inhibitor of pancreatic cancer cell survival. Mol.Cancer Res. 11 901 PMID: 23696131
If you know of a relevant reference for Mitoxantrone dihydrochloride, please let us know.
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Keywords: Mitoxantrone dihydrochloride, Mitoxantrone dihydrochloride supplier, topoisomerase, II, inhibitors, inhibits, DNA, type, antitumor, immunosuppressant, synthesis, repair, PIM1, kinase, USP11, ubiquitin, specific, peptidase, 11, chemotherapeutics, Topoisomerase, Pim, Kinase, Deubiquitinating, Enzymes, 4250, Tocris Bioscience
⚠ WARNING: This product can expose you to chemicals including Mitoxantrone hydrochloride, which is known to the State of California to cause cancer. For more information, go to www.P65Warnings.ca.gov
2 Citations for Mitoxantrone dihydrochloride
Citations are publications that use Tocris products. Selected citations for Mitoxantrone dihydrochloride include:
Zhang (2017) The BTK Inhibitor, Ibrutinib (PCI-32765) Overcomes PacT. Resistance in ABCB1 and ABCC10 Overexpressing Cells and Tumors. Mol Cancer Ther 16 1021 PMID: 28265007
Kathawala et al (2015) The small molecule tyrosine kinase inhibitor NVP-BHG712 antagonizes ABCC10-mediated PacT. resistance: a preclinical and pharmacokinetic study. Oncotarget 6 510 PMID: 25402202
Do you know of a great paper that uses Mitoxantrone dihydrochloride from Tocris? Please let us know.
Reviews for Mitoxantrone dihydrochloride
Average Rating: 5 (Based on 1 Review.)
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Paclitaxel, docetaxel, vincristine, vinblastine, colchicine, cisplatin, and mitoxantrone screen for Human epidermal carcinoma.
By
Anonymous on 11/17/2019
Assay Type: In Vitro
Species: Human
Cell Line/Tissue: Human epidermal carcinoma cell line
Human epidermal carcinoma cell line was treated with Paclitaxel, docetaxel,vincristine, vinblastine, colchicine, cisplatin, and mitoxantrone which purchased from Tocris Bioscience.
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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. Adapted from the 2015 Cancer Product Guide, Edition 3, 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.