货号:A316040
同义名:
CP-4055; CP 4055
CP 4055 (Elacytarabine) is a lipid-conjugated derivative of the nucleoside analog cytarabine. CP 4055 is an antineoplastic drug with cytotoxicity in solid tumors.
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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]. |
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 << |
计算器 | ||||
存储液制备 | ![]() |
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 |
CAS号 | 188181-42-2 |
分子式 | C27H45N3O6 |
分子量 | 507.66 |
SMILES Code | O=C(CCCCCCC/C=C\CCCCCCCC)OC[C@H]([C@@H](O)[C@@H]1O)O[C@H]1N2C=CC(N)=NC2=O |
MDL No. | MFCD19443751 |
别名 | CP-4055; CP 4055 |
运输 | 蓝冰 |
InChI Key | FLFGNMFWNBOBGE-FNNZEKJRSA-N |
Pubchem ID | 6438895 |
存储条件 |
In solvent -20°C:3-6个月-80°C:12个月 Pure form Keep in dark place, inert atmosphere, 2-8°C |
溶解方案 |
请根据您的动物给药指南选择适当的溶解方案。 以下溶解方案都请先按照体外实验的方式配制澄清的储备液,再依次添加助溶剂: ——为保证实验结果的可靠性,澄清的储备液可以根据储存条件,适当保存;体内实验的工作液,建议现用现配,当天使用; 以下溶剂前显示的百分比是指该溶剂在终溶液中的体积占比;如在配制过程中出现沉淀、析出现象,可以通过加热和/或超声的方式助溶
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