Voreloxin (SNS-595) hydrochloride

Catalog No.S7518 Synonyms: Vosaroxin

Voreloxin (SNS-595) hydrochloride Chemical Structure

Molecular Weight(MW): 437.9

Voreloxin is a potent Topoisomerase II inhibitor with broad-spectrum anti-tumor activity. Phase 2.

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Notes:

2. For more details, such as half maximal inhibitory concentrations (IC50s) and working concentrations of each inhibitor, please click on the link of the inhibitor of interest.
3. "+" indicates inhibitory effect. Increased inhibition is marked by a higher "+" designation.
4. Orange "√" refers to compounds which do inhibitory effects on the related isoform, but without specific value.

Biological Activity

Description Voreloxin 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

Cell Research
+ Expand
  • 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.
    (Only for Reference)
Animal Research
+ Expand
  • Animal Models: Mice implanted with P388 leukemia cells.
  • Formulation: Suspended in 0.4% CMC (carboxymethyl cellulose)
  • Dosages: ~50 mg/kg
  • Administration: i.p.
    (Only for Reference)

Solubility (25°C)

In vitro DMSO 1 mg/mL (2.28 mM)
Water 1 mg/mL (2.28 mM)
Ethanol <1 mg/mL
In vivo

* 1 mg/ml means slightly soluble or insoluble.
* Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations.

Chemical Information

Molecular Weight 437.9
Formula

C18H20ClN5O4S

CAS No. 175519-16-1
Storage powder
in solvent
Synonyms Vosaroxin

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Clinical Trial Information

NCT Number Recruitment Conditions Sponsor/Collaborators Start Date Phases
NCT02658487 Recruiting 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
NCT02485353 Recruiting Leukemia, Myeloid, Acute Hamid Sayar|Indiana University October 2015 --
NCT01913951 Recruiting Myelodysplastic Syndromes Washington University School of Medicine November 2013 Phase 1
NCT01980056 Recruiting Myelodysplastic Syndrome Weill Medical College of Cornell University|Sunesis Pharmaceuticals October 2013 Phase 1|Phase 2
NCT01893320 Active, not recruiting Leukemia M.D. Anderson Cancer Center|Sunesis Pharmaceuticals July 2013 Phase 1|Phase 2
NCT01191801 Active, not recruiting Leukemia|Acute Myeloid Leukemia|Acute Nonlymphocytic Leukemia Sunesis Pharmaceuticals October 2010 Phase 3

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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Topoisomerase Signaling Pathway Map

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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID