生物活性
内达铂是一种铂复合物,具有强大的抗肿瘤活性。奈达铂比其他含铂产品产生更少的恶心、呕吐和肾毒性。NDP作为第二代铂配合物被开发出来。因为它比顺铂(CDDP)具有更强的抗肿瘤活性和更低的肾毒性。奈达铂(NDP)是一种第二代铂复合物,具有较低的肾毒性,可替代CDDP或甚至超过CDDP与其他药物联合使用。
化学数据
分子量 | 303.17 |
分子式 | C2H8N2O3Pt |
CAS号 | 95734-82-0 |
纯度 | >98% |
溶解性(25°C) | DMSO water 10mg/mL |
储存和运输条件 | 固体粉末: -20°C 冷藏长期储存 常温运输及临时存放 |
实验操作 来自于公开的文献,仅供相同实验参考(如实验材料、目的不同,请参考其他文献)
细胞实验 |
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细胞系 | Human SCLC cell line SBC-3 and human NSCLC cell line PC-14 |
方法 | 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, exposing cells to drugs alone or in combination for 6 days at 37°C in an atmosphere of 100% humidity with 5% CO2; then pipetting the cells 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%. Defining the IC50 as the drug concentration required for a 50% reduction in the number of cells.Carrying four or five independent experiments out for each. Treating the cells 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 to check the effect of the drug treatment schedule on the effect of the combination . For the sequential exposure treatment, exposing cells to the first drug for 3 hours, ished in fresh medium once, and then immediately exposing to the second drug for 3 hours. Culturing the treated cells in drug-free medium until evaluation |
浓度 | 0.005 μg/mL, 0.01 μg/mL, 0.025 μg/mL, 0.05 μg/mL, 0.1 μg/mL, 0.25 μg/mL, and 0.5 μg/mL |
处理时间 | 6 days |
动物实验 |
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动物模型 | Tumor-bearing athymic BALB/c nude mice with Ma44 or NCI-H460 cells |
配制 | Saline |
剂量 | 10 mg/kg or 20 mg/kg |
给药处理 | Administered via i.v. |
不同实验动物依据体表面积的等效剂量转换表(数据来源于FDA指南)
| 小鼠 | 大鼠 | 兔 | 豚鼠 | 仓鼠 | 狗 |
重量 (kg) | 0.02 | 0.15 | 1.8 | 0.4 | 0.08 | 10 |
体表面积 (m2) | 0.007 | 0.025 | 0.15 | 0.05 | 0.02 | 0.5 |
Km系数 | 3 | 6 | 12 | 8 | 5 | 20 |
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,依据体表面积折算法,将化合物用于小鼠的剂量20 mg/kg 换算成大鼠的剂量,需要将20 mg/kg 乘以小鼠的Km系数(3),再除以大鼠的Km系数(6),得到化合物用于大鼠的等效剂量为10 mg/kg。
储备液配制
以下数据基于产品分子量,对于特殊产品,请参照COA中的储备液配制条件和说明进行操作。
Concentration / Solvent Volume / Mass | 1 mg | 5 mg | 10 mg |
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1 mM | 3.2985 mL | 16.4924 mL | 32.9848 mL |
5 mM | 0.6597 mL | 3.2985 mL | 6.597 mL |
10 mM | 0.3298 mL | 1.6492 mL | 3.2985 mL |