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9014-02-2

中文名称 NEOCARZINOSTATIN FROM STREPTOMYCEC CARZINOSTATICUS 来源于抑癌链霉菌
英文名称 NEOCARZINOSTATIN
CAS 9014-02-2
更新日期 2024/06/24 17:53:28
9014-02-2 结构式 9014-02-2 结构式

基本信息

中文别名
NEOCARZINOSTATIN FROM STREPTOMYCEC CARZINOSTATICUS 来源于抑癌链霉菌
英文别名
Aids002003
NSC-157365
a8544527g1
Aids-002003
neocarcinostatin
neocarzinostatink
NEOCARZINOSTATIN FROM STREPTOMYCEC CARZINOSTATICUS
neocarzinostatin from streptomyces carzinostaticus
所属类别
原料药:抗生素类药物

物理化学性质

熔点260° (dec)
储存条件2-8°C
形态Liquid
颜色Colorless to light yellow

常见问题列表

简介
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。
生物活性
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。
体外研究

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.

安全数据

毒性LD50 in mice (mg/kg): 1050 orally, 0.96 i.v. (Toriyama)
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