CAS NO: | 175519-16-1 |
规格: | ≥98% |
包装 | 价格(元) |
5mg | 电议 |
10mg | 电议 |
25mg | 电议 |
50mg | 电议 |
100mg | 电议 |
250mg | 电议 |
Molecular Weight (MW) | 437.9 |
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Formula | C18H20ClN5O4S |
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 info | Chemical 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 Key: XZAFZXJXZHRNAQ-STQMWFEESA-N 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[C@H](OC)[C@@H](NC)C4)=N3)C1=O)O |
Synonyms | Vosaroxin; SNS 595; SPC595; AG7352; SNS595; SPC-595; AG-7352; SNS-595; SPC 595; AG 7352; VVosaroxin |
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. |
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In Vivo | Voreloxin (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 model | Mice implanted with P388 leukemia cells. |
Formulation & Dosage | Dissolved in 0.4% CMC (carboxymethyl cellulose); 50 mg/kg; i.p. injection |
References | J Med Chem. 2004 Apr 8;47(8):2097-109; Cancer Chemother Pharmacol. 2009 Jun;64(1):53-65. |