Elacytarabine
产品说明书
 |
同义名 : | CP-4055; CP 4055 |
| CAS号 : | 188181-42-2 | |
| 货号 : | A316040 | |
| 分子式 : | C27H45N3O6 | |
| 纯度 : | 98%+ | |
| 分子量 : | 507.66 | |
| MDL号 : | MFCD19443751 | |
| 存储条件： |
Pure form Keep in dark place, inert atmosphere, 2-8°C In solvent -20°C:3-6个月-80°C:12个月 |
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| 溶解度 : | - | |
| 动物实验配方： |
| 生物活性 | |||
|---|---|---|---|
| 描述 | The clinical activity of cytarabine (ara-C) can be impaired by a deficient cellular drug uptake due to a reduced expression of nucleoside transporters in cancer cells. CP-4055, the 5’-elaidic acid esters of ara-C, has been synthesized to overcome the resistance caused by limited cellular uptake. Parental CEM cells presented a sensitivity to CP-4055 with a mean drug concentration resulting in 50% growth inhibition (GI50) of approximately 0.01 µM relative to untreated cells after 72 h treatment. CP-4055 induced high levels of annexin-V positive cells, while no apoptosis induction was observed after treatment of CEM/araC/8C cells with ara-C. Thus, the increase in cytotoxic activity observed after treatment of CEM/araC/8C cells with CP-4055 was principally because of an increase in apoptosis induction compared to the parental drug ara-C. Treatment of CEM cells with CP-4055 showed a classical arrest of cell cycle in the S-phase[1]. In preclinical and clinical studies, CP-4055 has demonstrated both safety and efficacy in acute myeloid leukemia (AML), with noteworthy activity among the cytarabine-refractory AML population[2]. | ||
| 临床研究 | |||||
|---|---|---|---|---|---|
| NCT号 | 适应症或疾病 | 临床期 | 招募状态 | 预计完成时间 | 地点 |
| NCT00232726 | Malignant Melanoma ... 展开 >> Neoplasm Metastasis 收起 << | Phase 2 | Completed | - | United States, Pennsylvania ... 展开 >> University of Pittsburgh Pittsburgh, Pennsylvania, United States, 15213-2584 Norway The Norwegian Radium Hospital Oslo, Norway, NO-0310 Sweden University Hospital Lund, Sweden, SE-221 85 收起 << |
| NCT01147939 | Acute Myeloid Leukemia (AML) | Phase 3 | Completed | - | - |
| NCT00498836 | Malignant Melanoma | Phase 2 | Completed | - | United States, Pennsylvania ... 展开 >> University of Pittsburgh Cancer Institute Pittsburgh, Pennsylvania, United States, 15232 United States, Texas Cancer Therapy and Research Center, Institute for Drug Development San Antonio, Texas, United States, 78229 Norway The Norwegian Radium Hospital Oslo, Norway, NO-0310 Sweden Lund University Hospital Lund, Sweden, SE-221 85 Umeå University Hospital Umeå, Sweden Uppsala University Hospital Uppsala, Sweden, SE-751 85 收起 << |
| 实验方案 | |||
|---|---|---|---|
| 1mg | 5mg | 10mg | |
|
1 mM 5 mM 10 mM |
1.97mL 0.39mL 0.20mL |
9.85mL 1.97mL 0.98mL |
19.70mL 3.94mL 1.97mL |
| 参考文献 |
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