Voreloxin (SNS-595)

Catalog No.S7518

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

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Voreloxin (SNS-595) Chemical Structure

Voreloxin (SNS-595) Chemical Structure
Molecular Weight: 401.44

Validation & Quality Control

Quality Control & MSDS

Product Information

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Product Description

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]
Features

Protocol(Only for Reference)

Cell Assay: [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 Study: [1]

Animal Models Mice implanted with P388 leukemia cells.
Formulation Suspended in 0.4% CMC (carboxymethyl cellulose)
Dosages ~50 mg/kg
Administration i.p.

Conversion of different model animals based on BSA (Value based on data from FDA Draft Guidelines)

SpeciesMouseRatRabbitGuinea pigHamsterDog
Weight (kg)0.020.151.80.40.0810
Body Surface Area (m2)0.0070.0250.150.050.020.5
Km factor36128520
Animal A (mg/kg) = Animal B (mg/kg) multiplied by  Animal B Km
Animal A Km

For example, to modify the dose of resveratrol used for a mouse (22.4 mg/kg) to a dose based on the BSA for a rat, multiply 22.4 mg/kg by the Km factor for a mouse and then divide by the Km factor for a rat. This calculation results in a rat equivalent dose for resveratrol of 11.2 mg/kg.

Rat dose (mg/kg) = mouse dose (22.4 mg/kg) ×  mouse Km(3)  = 11.2 mg/kg
rat Km(6)
1

References

[1] Tsuzuki Y, et al. J Med Chem. 2004, 47(8), 2097-2109.

[2] Hoch U, et al. Cancer Chemother Pharmacol. 2009, 64(1), 53-65.

Clinical Trial Information( data from http://clinicaltrials.gov, updated on 2016-07-30)

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|Mye  ...more 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  ...more 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 Pharm  ...more 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

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Chemical Information

Download Voreloxin (SNS-595) SDF
Molecular Weight (MW) 401.44
Formula

C18H19N5O4S

CAS No. 175414-77-4
Storage 3 years -20℃powder
2 years -80℃in solvent
Synonyms Vosaroxin
Solubility (25°C) * In vitro DMSO 1 mg/mL (2.49 mM)
Water 1 mg/mL (2.49 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 Name 1,8-Naphthyridine-3-carboxylic acid, 1,4-dihydro-7-[(3S,4S)-3-methoxy-4-(methylamino)-1-pyrrolidinyl]-4-oxo -1-(2-thiazolyl)-

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.

Tel: +1-832-582-8158 Ext:3

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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID
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