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    Voreloxin (SNS-595) HCl
    Voreloxin (SNS-595) HCl

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    This product is for research use only, not for human use. We do not sell to patients.
    Number: - + Pieces(InventoryPieces)
    InvivoChem Cat #: V1396
    CAS #: 175519-16-1Purity ≥98%

    Description: 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 investigational drug assigned with orphan status for treating acute myelogenous leukemia (AML) and ovarian cancer. It acts by intercalating into DNA in a site-specific manner and blocking the re-ligation process carried out by topoisomerase II during DNA replication. As a result, inhibition of DNA replication, RNA and protein synthesis occurs, followed by cell cycle arrest at G2 phase and induced p53-independent apoptosis.

    References: J Med Chem. 2004 Apr 8;47(8):2097-109; Cancer Chemother Pharmacol. 2009 Jun;64(1):53-65. 

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    Molecular Weight (MW)437.9
    CAS No.175519-16-1
    Storage-20℃ for 3 years in powder form
    -80℃ for 2 years in solvent
    Solubility (In vitro)DMSO: 1 mg/mL (2.3 mM)
    Water: 1 mg/mL (2.3 mM)
    Ethanol: <1 mg/mL
    Other infoChemical Name: 7-((3S,4S)-3-methoxy-4-(methylamino)pyrrolidin-1-yl)-4-oxo-1-(thiazol-2-yl)-1,4-dihydro-1,8-naphthyridine-3-carboxylic acid.
    InChi Code: InChI=1S/C18H19N5O4S/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)/t12-,13-/m0/s1
    SMILES Code: O=C(C1=CN(C2=NC=CS2)C3=C(C=CC(N4C[[email protected]](OC)[[email protected]@H](NC)C4)=N3)C1=O)O
    SynonymsVosaroxin; SNS 595; SPC595; AG7352; SNS595; SPC-595; AG-7352; SNS-595; SPC 595; AG 7352; VVosaroxin

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    In Vitro

    In vitro activity: 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. 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.

    Cell Assay: 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.

    In VivoVoreloxin (50 mg/kg i.p.) shows potent in vivo antitumor activity mice implanted with P388 leukemia cells. 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).
    Animal modelMice implanted with P388 leukemia cells.
    Formulation & DosageDissolved in 0.4% CMC (carboxymethyl cellulose); 50 mg/kg; i.p. injection
    ReferencesJ Med Chem. 2004 Apr 8;47(8):2097-109; Cancer Chemother Pharmacol. 2009 Jun;64(1):53-65. 

    These protocols are for reference only. InvivoChem does not independently validate these methods.


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