Voreloxin (SNS-595) hydrochloride

Catalog No.S7518 Synonyms: Vosaroxin

For research use only.

Voreloxin hydrochloride (SNS-595, Vosaroxin) is a potent Topoisomerase II inhibitor with broad-spectrum anti-tumor activity. Phase 2.

Voreloxin (SNS-595) hydrochloride Chemical Structure

CAS No. 175519-16-1

Selleck's Voreloxin (SNS-595) hydrochloride has been cited by 6 Publications

Purity & Quality Control

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Biological Activity

Description Voreloxin hydrochloride (SNS-595, Vosaroxin) is a potent Topoisomerase II inhibitor with broad-spectrum anti-tumor activity. Phase 2.
Targets
Topo II [1]
In vitro

Voreloxin exhibits potent inhibitory effect in topoisomerase II relaxation with IC50 of 3.2 μg /mL without effect on topoisomerase II cleavage. Voreloxin has a cytotoxic activity against human tumor cell lines more potent than that of etoposide. [1] Voreloxin has broad anti-proliferative activity in 15 cell lines, including 4 drug-resistant lines, with IC50 ranging from 0.04 to 1.155 μM. [2]

In vivo Voreloxin (50 mg/kg i.p.) shows potent in vivo antitumor activity mice implanted with P388 leukemia cells. [1] Voreloxin (25 mg/kg i.v.) demonstrates strong tumor growth inhibition in 10 of 11 solid tumor (breast, ovarian, colon, lung, gastric, and melanoma) xenograft models, 2 hematologic tumor xenograft models, 3 multidrug resistant tumor models and 3 murine syngeneic tumor models (Colon 26, Lewis Lung carcinoma, M5076 Ovarian Sarcoma). [2]

Protocol (from reference)

Cell Research:[1]
  • Cell lines: P388 leukemia cells
  • Concentrations: ~10 μg/mL
  • Incubation Time: 72 hours
  • Method: Cells are put into wells of a 96-well microtiter plate in the amount of 0.1 mL/well, preincubated for 24 h except for P388 cells, and incubated with various concentrations of a test compound in the 5% CO2 incubator at 37 ° for 72 h. After the culturing, 0.02 mL of a MTT solution (5 mg/mL) is put in each well, and the cells are cultured for a further 4 h. The medium is removed by suction, and 0.2 mL of DMSO is put in each well to dissolve the formed formazan. The absorbance is measured by Multiskan Bichromatic. The IC50 is defined as the drug concentration needed to produce a 50% reduction of absorbance relative to the control.
Animal Research:[1]
  • Animal Models: Mice implanted with P388 leukemia cells.
  • Dosages: ~50 mg/kg
  • Administration: i.p.

Solubility (25°C)

In vitro

Chemical Information

Molecular Weight 437.9
Formula

C18H20ClN5O4S

CAS No. 175519-16-1
Storage 3 years -20°C powder
2 years -80°C in solvent
Smiles CNC1CN(CC1OC)C2=NC3=C(C=C2)C(=O)C(=CN3C4=NC=CS4)C(=O)O.Cl

In vivo Formulation Calculator (Clear solution)

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Method for preparing in vivo formulation: Take μL DMSO master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O, mix and clarify.

Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.

Note: 1. Please make sure the liquid is clear before adding the next solvent.
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Molarity Calculator

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Clinical Trial Information

NCT Number Recruitment Interventions Conditions Sponsor/Collaborators Start Date Phases
NCT02658487 Active not recruiting Drug: Cytarabine|Drug: Vosaroxin Acute Myeloid Leukemia|Acute Myeloid Leukemia Arising From Previous Myelodysplastic Syndrome|Acute Myeloid Leukemia With Multilineage Dysplasia|Myeloid Sarcoma|Secondary Acute Myeloid Leukemia|Therapy-Related Acute Myeloid Leukemia|Therapy-Related Myelodysplastic Syndrome Vanderbilt-Ingram Cancer Center|National Cancer Institute (NCI) March 2016 Phase 2
NCT01913951 Active not recruiting Drug: vosaroxin|Drug: Azacitidine Myelodysplastic Syndromes Washington University School of Medicine|Sunesis Pharmaceuticals November 22 2013 Phase 1
NCT01980056 Completed Drug: Vosaroxin Myelodysplastic Syndrome Weill Medical College of Cornell University|Sunesis Pharmaceuticals October 25 2013 Phase 1|Phase 2
NCT01893320 Completed Drug: Vosaroxin|Drug: Decitabine Leukemia M.D. Anderson Cancer Center|Sunesis Pharmaceuticals July 18 2013 Phase 1|Phase 2

(data from https://clinicaltrials.gov, updated on 2022-01-17)

Tech Support

Answers to questions you may have can be found in the inhibitor handling instructions. Topics include how to prepare stock solutions, how to store inhibitors, and issues that need special attention for cell-based assays and animal experiments.

Handling Instructions

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