包装 | 价格(元) |
10mM (in 1mL DMSO) | 电议 |
5mg | 电议 |
10mg | 电议 |
25mg | 电议 |
Cell lines | SK-BR-3, ScaBER, PANC-1, KB, HCT116, SKOV3, GT3TKB, Hs746T, Calu-6, NCI-H460, PA-1, MES-SA, SBC-3, SBC-3/ETP and PC-14 cells |
Preparation method | The solubility of this compound in DMSO is >10 mM. General tips for obtaining a higher concentration: Please warm the tube at 37℃ for 10 minutes and/or shake it in the ultrasonic bath for a while. Stock solution can be stored below -20℃ for several months. |
Reaction Conditions | 0.04 ~ 1.155 μM; 72 hrs |
Applications | Voreloxin exhibited broad anti-proliferative activity in 15 cell lines, including 4 drug-resistant lines, with the IC50 values ranging from 0.04 to 1.155 μM. |
Animal models | Mice implanted with P388 leukemia cells |
Dosage form | 3.13, 12.5 or 50 mg/kg; i.p.; on days 1 and 5 after tumor implantation |
Applications | In mice implanted with P388 leukemia cells, Voreloxin (50 mg/kg, i.p.) showed potent antitumor activity. |
Other notes | Please test the solubility of all compounds indoor, and the actual solubility may slightly differ with the theoretical value. This is caused by an experimental system error and it is normal. |
产品描述 | 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 treatment of 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]. Clinical trial: Voreloxin showed an acceptable safety profile with clinical activity in patients with relapsed/refractory solid tumors. The maxmum tolerence dose was schedule-dependent. Voreloxin is now in clinical studies of ovarian cancer and acute myeloid leukemia [3]. References: |