生物活性
Docetaxel是一种紫杉醇类似物，通过结合到稳定的微管来抑制微管解聚。Docetaxel是一种细胞毒性剂，尤其对于增殖细胞，Docetaxel促进微管蛋白束的形成，还能诱导持续的有丝分裂阻滞，随后分裂阻滞的细胞凋亡或永久抑制分裂。
Docetaxel抑制微管的动态不稳定性及踏车现象，导致染色体不能分开到子细胞中，这样又会反过来触发有丝分裂过早结束，而不是在细胞周期的特定时期进行抑制作用。 Docetaxel (150 ng/mL) 处理人类小细胞肺癌 N417细胞系 1小时，抑制50% 细胞生长。
化学数据
| 分子量 | 807.88 |
| 分子式 | C43H53NO14 |
| CAS号 | 114977-28-5 |
| 纯度 | 98.36% |
| 溶解性（25°C） | DMSO 60 mg/mL
Ethanol 60 mg/mL |
| 储存和运输条件 | 2-8°C, protect from light, dry, sealed
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 |
|---|
| 细胞系 | A549, HCT-116, NCI-H838, KB-3-1, MX-1W, NCI-H1299 and DLD-1 cells |
| 方法 | Cell Proliferation Assays
Cytotoxicity was assessed by growing cells in the presence of agents for 72 h. Cell survival was measured by the sulforhodamine B (SRB) protein stain method or the ATP-binding assay using the Cell-Titer Glo Luminescent Reporter (GLR) System (Promega, Inc., Madison, WI). The SRB assay was done as previously described (23). For the GLR system, cells were plated robotically at approximately 50% confluency in a 384-well plate and allowed to attach for 12 h at 37°C/5% CO2. After diluting test agents using BioMek 2000 robotic system (Beckman Instruments, Fullerton, CA), agents were added to each well and incubated for 72 h. ATP binding and stabilization of the luminescent signal were performed according to manufacturer's protocol (Promega) following tumor cell lysis. Absorbance was read on a Victor V multilabel plate reader (Perkin-Elmer, Gaithersburg, MD) at a wavelength of A595 and data collected using Wallac 1420 Workstation software. |
| 浓度 | 0~100 nM |
| 处理时间 | 72 h |
| 动物实验 |
|---|
| 动物模型 | Athymic nu/nu female mice bearing Lox melanoma cells, KB-3-1 cells and A375SM melanoma cells tumour xenograft model |
| 配制 | 1.4% ethanol/3.5% polysorbate 80 in saline |
| 剂量 | 25 mg/kg |
| 给药处理 | 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 |
|---|
| 1 mM | 1.2378 mL | 6.189 mL | 12.3781 mL |
| 5 mM | 0.2476 mL | 1.2378 mL | 2.4756 mL |
| 10 mM | 0.1238 mL | 0.6189 mL | 1.2378 mL |
m.cnreagent.com