175414-77-4 Usage
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.
Check Digit Verification of cas no
The CAS Registry Mumber 175414-77-4 includes 9 digits separated into 3 groups by hyphens. The first part of the number,starting from the left, has 6 digits, 1,7,5,4,1 and 4 respectively; the second part has 2 digits, 7 and 7 respectively.
Calculate Digit Verification of CAS Registry Number 175414-77:
(8*1)+(7*7)+(6*5)+(5*4)+(4*1)+(3*4)+(2*7)+(1*7)=144
144 % 10 = 4
So 175414-77-4 is a valid CAS Registry Number.
175414-77-4Relevant articles and documents
STABLE SNS-595 COMPOSITIONS AND METHODS OF PREPARATION
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Page/Page column 24; 58, (2011/04/14)
Methods of preparing substantially pure SNS-595 substance are disclosed. Also provided are compositions comprising SNS-595 substance that are substantially pure and essentially free of visible particles.
METHOD OF PREPARING (+)-1,4-DIHYDRO-7-[(3S,4S)-3METHOXY-4-(METHYLAMINO)-1-PYRROLIDINYL]-4-OXO-1-(2-THIAZOLYL)-1,8-NAPHTHYRIDINE-3-CARBOXYLIC ACID
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Page/Page column 54, (2010/08/04)
Methods of preparing (+)-1, 4-dihydro-7-[(3S,45)-3-methoxy-4-(methylamino)-1 - pyrrolidinyl]-4-oxo-1-(2-thiazolyl)-1,8-naphthyridine-3-carboxylic acid are disclosed. Also provided are pharmaceutical compositions comprising (+)-1,4-dihydro-7-[(3S,4S)-3-methoxy-4-(methylamino)-1-pyrrolidinyl]-4-oxo-1-(2-thiazolyl)-1,8-naphthyridine-3-carboxylic acid, and methods of treatment using such compositions.
Compounds, processes for the preparation thereof and anti-tumor agents
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, (2008/06/13)
This invention relates to pyridone-carboxylic acid derivatives of the following formula or salts thereof: STR1 wherein R1 is a hydrogen atom, a halogen atom, etc., R2 is a carboxyl group etc., R3 is a hydrogen atom etc., A
