CAS NO: | 175414-77-4 |
包装 | 价格(元) |
100mg | 电议 |
250mg | 电议 |
500mg | 电议 |
生物活性 | Voreloxin (SNS-595; Vosaroxin; AG 7352) is a first-in-classtopoisomeraseIIinhibitor that intercalates DNA and induces site-selective DNA DSB, G2 arrest, andapoptosis. | |
IC50& Target |
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体外研究 (In Vitro) | 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[1]. 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[2]. Voreloxin is active on the primary acute myeloid leukemia (AML) with a mean LD50of 2.3 μM. The LD50for 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[3]. | |
体内研究 (In Vivo) | 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[2]. | |
Clinical Trial | ||
分子量 | 401.44 | |
Formula | C18H19N5O4S | |
CAS 号 | 175414-77-4 | |
运输条件 | Room temperature in continental US; may vary elsewhere. | |
储存方式 | Please store the product under the recommended conditions in the Certificate of Analysis. |