Voreloxin

Voreloxin Basic information
Product Name:Voreloxin
Synonyms:1,8-Naphthyridine-3-carboxylic acid, 1,4-dihydro-7-[(3S,4S)-3-methoxy-4-(methylamino)-1-pyrrolidinyl]-4-oxo -1-(2-thiazolyl)-;Voreloxin (SNS-595);Voreloxin, >=98%;Voreloxin;AG-7352;SNS-595;SPC-595;AG-7352, 1,4-dihydro-7-[(S,S)-3-Methoxy-4-MethylaMino-1-pyrrolidinyl]-4-oxo-1-(2-thiazolyl)-1,8-naphthyridine-3-carboxylic, (+)-1,4-dihydro-7-[(3S,4S)-3-Methoxy-4-(MethylaMino)-1-pyrrolidinyl]-4-oxo-1-(2-thiazolyl)-1,8-naphthyridine-3-carboxylic acid
CAS:175414-77-4
MF:C18H19N5O4S
MW:401.44
EINECS:
Product Categories:API;Inhibitors
Mol File:175414-77-4.mol
Voreloxin Structure
Voreloxin Chemical Properties
Boiling point 652.0±65.0 °C(Predicted)
density 1.52±0.1 g/cm3(Predicted)
storage temp. Store at -20°C
solubility insoluble in H2O; insoluble in EtOH; insoluble in DMSO
form solid
pka5.68±0.70(Predicted)
Safety Information
MSDS Information
Voreloxin Usage And Synthesis
UsesVoreloxin is a potent Topoisomerase II inhibitor with broad-spectrum anti-tumor activity.
Biological Activityvoreloxin, formerly known as sns-595 or ag-7352, is a novel naphthyridine analog, which is structurally related to the quinolone antibiotics, a chemical class not previously used for the treatmentof cancer.
in vitroin vitro studies demonstrated voreloxin has broad anti-proliferative activity in 11 tumor cell lines, with ic50 values ranging from 0.04 to 0.97 μm. similar activity was observed in vitro in drug-resistant cell lines, including those that overexpress p-glycoprotein [2].
in vivoafter a single intravenous dose, voreloxin concentrations in tumor were correlated with induction of the apoptosis marker caspase-3. administration of voreloxin at 20 mg/kg weekly inhibited tumor growth (86%). voreloxin demonstrated strong dose-dependent tumor growth inhibition (63–88%) in 10 of 11 solid tumor xenograft models [2].
references[1] tsuzuki y, tomita k, shibamori k, sato y, kashimoto s, chiba k. synthesis and structure-activity relationships of novel 7-substituted 1,4-dihydro-4-oxo-1-(2-thiazolyl)-1,8-naphthyridine-3-carboxylic acids as antitumor agents. part 2. j med chem. 2004;47(8):2097-109.
[2] hoch u, lynch j, sato y, kashimoto s, kajikawa f, furutani y, silverman ja. voreloxin, formerly sns-595, has potent activity against a broad panel of cancer cell lines and in vivo tumor models. cancer chemother pharmacol. 2009;64(1):53-65.
[3] advani rh, hurwitz hi, gordon ms, ebbinghaus sw, mendelson ds, wakelee ha, hoch u, silverman ja, havrilla na, berman cj, fox ja, allen rs, adelman dc. voreloxin, a first-in-class anticancer quinolone derivative, in relapsed/refractory solid tumors: a report on two dosing schedules. clin cancer res. 2010;16(7):2167-75.
Voreloxin Preparation Products And Raw materials
BEZ235 (NVP-BEZ235, Dactolisib) Ganetespib Rapamycin Ibrutinib Vorapaxar Cyclophosphamide monohydrate Panobinostat PVM/MA Vorapaxar Sulfate GS9857

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