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5mg |
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10mg |
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25mg |
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50mg |
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100mg |
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250mg |
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Purity: ≥98%
Voreloxin HCl (formerly known as AG-7352; SNS-595; SPC 595; AG 7352; SNS595, AG-7352; Vosaroxin), the hydrochloride salt of Voreloxin which is a naphthyridine analog, is a novel and potent Topoisomerase II inhibitor with a broad-spectrum antineoplastic activity. Vosaroxin is an experimental medication that has been given orphan status to treat ovarian cancer and acute myelogenous leukemia (AML). It works by selectively intercalating into DNA to obstruct topoisomerase II's re-ligation process during DNA replication. The result is the inhibition of RNA, protein, and DNA replication, which is followed by cell cycle arrest at the G2 phase and p53-independent apoptosis.
Targets |
Topoisomerase II
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ln Vitro |
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ln Vivo |
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Cell Assay |
MTS cell proliferation assays are used to conduct in vitro toxicity tests on primary AML mononuclear cells over the course of 48 hours. One can calculate lethal doses (LD50). In a final volume of 90 μL, cells are treated with voreloxin (31.25 nM to 4 μM) and Ara-C (62.5 nM to 8 μM) by serial dilution and incubated for 48 hours. After incubation, the reaction is incubated for an additional 4 hours with the addition of 20 μL of MTS reagent. Spectrophotometry is used to measure the absorbance of the reaction at 490 nm after this point, and the percentage of viable cells is computed in relation to the untreated control cells in the same experiment. Software called Calcusyn is used to calculate IC50 values[3].
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Animal Protocol |
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References |
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Molecular Formula |
C18H20CLN5O4S
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Molecular Weight |
437.9
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Exact Mass |
437.09
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CAS # |
175519-16-1
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Related CAS # |
175414-77-4
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Appearance |
Powder
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SMILES |
CN[C@H]1CN(C[C@@H]1OC)C2=NC3=C(C=C2)C(=O)C(=CN3C4=NC=CS4)C(=O)O.Cl
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InChi Key |
JJZCCQHWCOXGCL-QNTKWALQSA-N
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InChi Code |
InChI=1S/C18H19N5O4S.ClH/c1-19-12-8-22(9-13(12)27-2)14-4-3-10-15(24)11(17(25)26)7-23(16(10)21-14)18-20-5-6-28-18;/h3-7,12-13,19H,8-9H2,1-2H3,(H,25,26);1H/t12-,13-;/m0./s1
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Chemical Name |
7-[(3S,4S)-3-methoxy-4-(methylamino)pyrrolidin-1-yl]-4-oxo-1-(1,3-thiazol-2-yl)-1,8-naphthyridine-3-carboxylic acid;hydrochloride
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Synonyms |
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Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month |
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Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
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Solubility (In Vitro) |
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Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
1 mM | 2.2836 mL | 11.4181 mL | 22.8363 mL | |
5 mM | 0.4567 mL | 2.2836 mL | 4.5673 mL | |
10 mM | 0.2284 mL | 1.1418 mL | 2.2836 mL |
*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.
Calculation results
Working concentration: mg/mL;
Method for preparing DMSO stock solution: mg drug pre-dissolved in μL DMSO (stock solution concentration mg/mL). Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug.
Method for preparing in vivo formulation::Take μL DMSO stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O,mix and clarify.
(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
(2) Be sure to add the solvent(s) in order.
Voreloxin combined with cytarabine has additive or synergistic activity in acute leukemia cell lines Viability studies were performed using human acute leukemia cell lines MV4-11, HL-60, and CCRF-CEM exposed for 72 h to serially diluted voreloxin and/or cytarabine. Cancer Chemother Pharmacol . 2010 Oct;66(5):881-8. td> |
Voreloxin and cytarabine, alone or in combination, ablate normal bone marrow CD-1 mice received vehicle, voreloxin, cytarabine, or voreloxin and cytarabine in combination on day 0 and 4. On day 6, femurs were isolated, and cellularity was assessed in H&E stained bone marrow sections. Cancer Chemother Pharmacol . 2010 Oct;66(5):881-8. td> |
The effect of voreloxin on cell cycle distribution was investigated by flow cytometry in (A) NB4 and (B) HL-60 cells following 12 h of treatment. Haematologica . 2011 Mar;96(3):393-9 td> |
Synergy between voreloxin and Ara-C was investigated in 25 primary AML samples over 48 h in vitro. Haematologica . 2011 Mar;96(3):393-9. td> |