CX-3543 is a fluoroquinolone derivative with antineoplastic activity. Quarfloxin disrupts the interaction between the nucleolin protein and a G-quadruplex DNA structure in the ribosomal DNA (rDNA) template, a critical interaction for rRNA biogenesis that is overexpressed in cancer cells; disruption of this G-quadruplex DNA:protein interaction in aberrant rRNA biogenesis may result in the inhibition of ribosome synthesis and tumor cell apoptosis.
CX-3543 is a fluoroquinolone derivative with antineoplastic activity. Quarfloxin disrupts the interaction between the nucleolin protein and a G-quadruplex DNA structure in the ribosomal DNA (rDNA) template, a critical interaction for rRNA biogenesis that is overexpressed in cancer cells; disruption of this G-quadruplex DNA:protein interaction in aberrant rRNA biogenesis may result in the inhibition of ribosome synthesis and tumor cell apoptosis.
动物 A (mg/kg) = 动物 B (mg/kg)×动物 B的Km系数/动物 A的Km系数 | |
例如,已知某工具药用于小鼠的剂量为88 mg/kg , 则用于大鼠的剂量换算方法:将88 mg/kg 乘以小鼠的Km系数(3),再除以大鼠的Km系数(6),得到该药物用于大鼠的等效剂量44 mg/kg。
[1] Drygin D.et al. Anticancer activity of CX-3543: a direct inhibitor of rRNA biogenesis.Cancer Res. 2009 Oct 1;69(19):7653-61. doi: 10.1158/0008-5472.CAN-09-1304.
分子式 C35H33FN6O3 |
分子量 604.67 |
CAS号 865311-47-3 |
储存方式 ﹣20 ℃冷藏长期储存。冰袋运输 |
溶剂(常温) |
DMSO 20 mg/mL |
Water <1 mg/mL |
Ethanol <1 mg/mL |
体内溶解度
NCT Number | Conditions | Interventions | Sponsor/Collaborators | Phases | Start Date | Last Updated |
NCT00955786 | Advanced Solid Tumors|Lymphoma | Drug: CX-3543 | Cylene Pharmaceuticals | Phase 1 | 2005-07-01 | 2009-08-07 |
NCT00780663 | Neuroendocrine Tumors|Carcinoid Tumor | Drug: Quarfloxin | Cylene Pharmaceuticals | Phase 2 | 2008-10-01 | 2011-06-13 |
NCT00485966 | B-Cell Chronic Lymphocytic Leukemia | Drug: CX-3543 | Cylene Pharmaceuticals | Phase 2 | 2007-06-01 | 2008-11-03 |
NCT00955292 | Advanced Solid Tumors|Lymphoma | Drug: Quarfloxin | Cylene Pharmaceuticals | Phase 1 | 2007-07-01 | 2009-08-07 |
注:以上所有数据均来自公开文献,并不保证对所有实验均有效,数据仅供参考。
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