|
| 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 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 | pka | 5.68±0.70(Predicted) |
| Voreloxin Usage And Synthesis |
Uses | Voreloxin is a potent Topoisomerase II inhibitor with broad-spectrum anti-tumor activity. | Biological Activity | voreloxin, 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 vitro | in 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 vivo | after 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 |
|