新制癌菌素
| 中文名称 | 新制癌菌素 |
|---|---|
| 中文同义词 | 新制癌菌素;NEOCARZINOSTATIN FROM STREPTOMYCEC CARZINOSTATICUS 来源于抑癌链霉菌 |
| 英文名称 | NEOCARZINOSTATIN |
| 英文同义词 | neocarcinostatin;neocarzinostatink;neocarzinostatin from streptomyces carzinostaticus;NSC-157365;Aids002003;Aids-002003;a8544527g1;NEOCARZINOSTATIN FROM STREPTOMYCEC CARZINOSTATICUS |
| CAS号 | 9014-02-2 |
| 分子式 | |
| 分子量 | 0 |
| EINECS号 | |
| 相关类别 | 对照品 |
| Mol文件 | Mol File |
| 结构式 |
新制癌菌素 性质
| 熔点 | 260° (dec) |
|---|---|
| 储存条件 | 2-8°C |
新制癌菌素(简称 NCS)是 1 种临床抗癌抗生素，由制癌链霉菌（Streptomyces carzinostaticus）产生，它是双烯二炔类抗癌抗生素色蛋白家族中的一员，由非蛋白生色团(NCS-C)和载体蛋白(Apo-NCS)组成。它的抗肿瘤功能源于蛋白质释放的生色团。Neocarzinostatin 是一种有效的 DNA 损伤的、抗肿瘤抗生素，可识别双链 DNA 膨胀并诱导DNA双链断裂 (DSBs)。Neocarzinostatin 诱导细胞凋亡 (apoptosis)。Neocarzinostatin 具有用于 EpCAM 阳性肿瘤的潜力。
The EpCAM aptamer conjugated Neocarzinostatin (NCS) shows specificity to EpCAM-positive cells. The effects of the conjugates on cancer cells are impressive as the conjugate arrests the cell cycle and promoted apoptosis and necrosis. The high levels of PARP expression confirmed the DNA breaks upon conjugate treatment. NCS conjugated with EpCAM can be targeted to cancer cells sparing normal cells.
The IC
50
values of Neocarzinostatin (72 hours) to C6 cells and U87MG cells were 493.64 nM, 462.96 nM, respectively.
In human tumor cell lines of different tissue origins, sensitivity to neocarzinostatin is proportional to the product of the relative contents of Bcl-2 and caspase-3.
安全信息
| 毒性 | LD50 in mice (mg/kg): 1050 orally, 0.96 i.v. (Toriyama) |
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