Nedaplatin 是顺铂的衍生物,是肿瘤集落形成单位的 DNA 损伤剂,IC50为94 μM。
产品描述
Nedaplatin is a derivative of cisplatin and DNA damage agent for tumor colony forming units (IC50: 94 μM). Containing a novel ring structure in which glycolate is bound to the platinum by a bidentate ligand, nedaplatin forms reactive platinum complexes that bind to nucleophilic groups in DNA, resulting in intrastrand and interstrand DNA cross-links, apoptosis and cell death.
体外活性
与这三种药物单独使用相比,在Nedaplatin或顺铂(FN或FC治疗)之前先连续使用5-FU给药对对肿瘤生长的抑制及存活时间的延长上具有协同加强作用.
体内活性
Nedaplatin (Aqupla)是顺铂衍生物,能抑制肿瘤克隆集落形成(IC50:28.5 μg/mL)。0.005-0.5 μg/mL的Nedaplatin对SBC-3细胞增殖的抑制效果为2%-98%(IC50:0.053 μg/mL)。
细胞实验
The inhibition of cell (including human SCLC cell line SBC-3 and human NSCLC cell line PC-14) proliferation after drug treatments as the antitumor activity using a regrowth assay is messured. Briefly, cells are exposed to drugs alone or in combination for 6 days at 37°C in an atmosphere of 100% humidity with 5% CO2; the cells are then pipetted six to eight times until almost all cells appeared as single cells and counted with a counter. For each drug, concentration-effect curves are drawn as plots of the fraction of surviving cells (unaffected cell fraction, fu) versus drug concentration. The cell proliferation ratio of the treated:control cultures (T:C%) is calculated as follows: [(the number of treated cells on day 6)/(the number of treated cells on day 0)]/[(the number of control cells on day 6)/(the number of control cells on day 0)] × 100%. The IC50 is defined as the drug concentration required for a 50% reduction in the number of cells. Four or five independent experiments are carried out for each. To check the effect of the drug treatment schedule on the effect of the combination, the cells are treated either by simultaneous exposure to the two drugs or by sequential exposure to Nedaplatin followed by irinotecan (Nedaplatin→irinotecan) and vice versa (irinotecan→Nedaplatin) for 3 hours. For the sequential exposure treatment, cells are exposed to the first drug for 3 hours, ished in fresh medium once, and then immediately exposed to the second drug for 3 hours. The treated cells are cultured in drug-free medium until evaluation.(Only for Reference)
Cas No.
95734-82-0
分子式
C2H8N2O3Pt
分子量
303.181
别名
奈达铂;NSC 375101D
储存和溶解度
H2O:10 mM
DMSO:Insoluble
Powder: -20°C for 3 years
In solvent: -80°C for 2 years