Voreloxin Inhibitor CAS No. 175414-77-4

Cat. No.	Name	Size	Price	Add Cart
KI1086	Voreloxin	5 mg	$550

Chemical Characteristic

Product Name	Voreloxin
Synonyms	SNS-595, Vosaroxin,AG 7352
CAS No.	175414-77-4
Molecular Weight	401.44
Formula	C₁₈H₁₉N₅O₄S
Chemical Name	1,8-Naphthyridine-3-carboxylic acid, 1,4-dihydro-7-[(3S,4S)-3-methoxy-4-(methylamino)-1-pyrrolidinyl]-4-oxo -1-(2-thiazolyl)-
Smiles	c1(cc(c(=O)n2ccccc12)C(=O)O)CN1CCN(CC1)c1ccc(cc1)C#N
Chemical Structure

Biological activities

Voreloxin is a first-in-class topoisomerase II inhibitor. Voreloxin intercalates DNA and induces site-selective DNA double-strand breaks (DSB), G2 arrest, and apoptosis.^[1] Voreloxin inhibits human tumor cell lines ovarian carcinoma PA-1, uterus sarcoma MES-SA and small-cell lung carcinoma SBC-3 with IC50 of 40, 96 and 79 nM, respectively. ^[2] Voreloxin also inhibits AML cell lines MV4-11 and HL-60 with average IC50 of 95 and 884 nM, respectively. ^[3] Administration of voreloxin at the dose of 20 mg/kg weekly effectively inhibits tumor (including breast MDA-MB-231, melanoma SK-MEL-5) growth. Voreloxin exhibits strong dose-dependent tumor growth inhibition (63??8%) in 10 of 11 solid tumor (breast, ovarian, colon, lung, gastric, and melanoma) xenograft models and three murine syngeneic tumor (Colon 26, Lewis Lung carcinoma, M5076 Ovarian Sarcoma) models. ^[2] Administration of voreloxin at MTD, 20 mg/kg q4d?2, results in an 80% reduction in cellularity relative to vehicle 2 days after treatment. ^[3]

Protocols

Voreloxin is dissolved in 4.5% sorbitol containing 0.17% methanesulfonic acid and further diluted with 5% sorbitol containing 0.02% methanesulfonic acid to obtain dosing solutions with the required concentrations. ^[2]

References

[1] Hawtin RE, et al. Voreloxin is an anticancer quinolone derivative that intercalates DNA and poisons topoisomerase II. PLoS One. 2010, 5(4): e10186. [2] Hoch U, et al. 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] Scatena CD, et al. Voreloxin, a first-in-class anticancer quinolone derivative, acts synergistically with cytarabine in vitro and induces bone marrow aplasia in vivo. Cancer Chemother Pharmacol. 2010, 66(5): 881-888.

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