| 货号 | 规格 | 价格 | 上海 | 北京 | 珠海 | 重庆 | 武汉 | 购买数量 |
|---|---|---|---|---|---|---|---|---|
Y28832-1mg促销 |
￥454.00 ￥360.00 |
10 | - | - | - | - |
|
|
Y28832-5mg促销 |
￥1260.00 ￥1010.00 |
10 | - | - | - | - |
|
|
Y28832-10mg促销 |
￥2020.00 ￥1610.00 |
10 | - | - | - | - |
|
|
Y28832-25mg促销 |
￥4080.00 ￥3260.00 |
3 | - | - | - | - |
|
|
Y28832-50mg促销 |
￥6520.00 ￥5220.00 |
3 | - | - | - | - |
|
|
Y28832-100mg促销 |
￥10400.00 ￥8350.00 |
1 | - | - | - | - |
|
| 产品描述： | Voreloxin (SNS-595; Vosaroxin; AG 7352) is a first-in-class topoisomerase II inhibitor that intercalates DNA and induces site-selective DNA DSB, G2 arrest, and apoptosis | ||||||||||||||||||||
|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|
| 靶点： | Topoisomerase II;Apoptosis; Topoisomerase | ||||||||||||||||||||
| 体外研究： | Voreloxin is a first-in-class topoisomerase II poison and inhibitor that intercalates DNA and induces site-selective DNA DSB, G2 arrest, and apoptosis. Voreloxin (0.1-20 µM) inhibits topoisomerase II activity and induces site-selective DNA DSB in CCRF-CEM cells. Voreloxin (0.11, 0.33, 1, 3 µM) induces G2 arrest partially through topoisomerase II in A549 lung cancer cell line. Voreloxin cytotoxic activity requires DNA intercalation. However, Voreloxin (1-9 µM) does not generate significant levels of ROS. Voreloxin has potent cytotoxic activity in AML cell lines MV4-11 and HL-60, with IC50s of 95 ± 8 nM and 884 ± 114 nM, respectively. Voreloxin in combination with cytarabine shows additive or synergistic activity in acute leukemia cell lines. Voreloxin is active on the primary acute myeloid leukemia (AML) with a mean LD50 of 2.3 μM. The LD50 for voreloxin in myeloid cell lines NB4 and HL-60 is 0.59 μM ± 0.25 μM. Voreloxin causes accumulation of cells in the S and G2 phases of the cell cycle and acts on topoisomerase II. | ||||||||||||||||||||
| 体内研究： | Voreloxin (20 mg/kg, i.v.) alone results in 80% reduction in bone marrow cellularity of CD-1 mice by administration one dose every 4 days repeated twice (q4d ×2). voreloxin at 10 mg/kg in combination with cytarabine causes ablation of the marrow, dilation of sinusoids, and infiltration of adipocytes in mice. Voreloxin (20 mg/kg, i.v.) combined with cytarabine causes a reversible decrease in myeloid and lymphoid cells in bone marrow and peripheral blood CD-1 mice. voreloxin (10 mg/kg, q4d ×2) and cytarabine in combination causes reversible neutropenia with a more modest impact on platelets CD-1 mice. | ||||||||||||||||||||
| 细胞实验： | 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. |
||||||||||||||||||||
| 动物实验： | 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. | ||||||||||||||||||||
| 参考文献： | 1. Hotinski AK, et al. Vosaroxin is a novel topoisomerase-II inhibitor with efficacy in relapsed and refractory acute myeloid leukaemia. Expert Opin Pharmacother. 2015 Jun;16(9):1395-402. 2. 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 Oct;66(5):881-8. 3. Walsby EJ, et al. The topoisomerase II inhibitor voreloxin causes cell cycle arrest and apoptosis in myeloid leukemia cells and acts in synergy with cytarabine. Haematologica. 2011 Mar;96(3):393-9. | ||||||||||||||||||||
| 溶解性： | Soluble in DMSO, not in water | ||||||||||||||||||||
| 保存条件： | -20℃ | ||||||||||||||||||||
| 配置溶液浓度参考： |
|
||||||||||||||||||||
| 注意： | 部分产品我司仅能提供部分信息，我司不保证所提供信息的权威性，仅供客户参考交流研究之用。 |
上海工商
沪公网安备 31011702002021号
危险品化学品经营许可证（不带存储）
营业执照(三证合一)
