9014-02-2
中文名稱
NEOCARZINOSTATIN FROM STREPTOMYCEC CARZINOSTATICUS 來源于抑癌鏈霉菌
英文名稱
NEOCARZINOSTATIN
CAS
9014-02-2
更新日期
2024/06/24 17:53:28
基本信息
中文別名
NEOCARZINOSTATIN FROM STREPTOMYCEC CARZINOSTATICUS 來源于抑癌鏈霉菌 英文別名
Aids002003NSC-157365
a8544527g1
Aids-002003
neocarcinostatin
neocarzinostatink
NEOCARZINOSTATIN FROM STREPTOMYCEC CARZINOSTATICUS
neocarzinostatin from streptomyces carzinostaticus
所屬類別
原料藥：抗生素類藥物物理化學(xué)性質(zhì)
熔點(diǎn)260° (dec)
儲(chǔ)存條件2-8°C
形態(tài)Liquid
顏色Colorless to light yellow
InChIKeyBLXZMHNVKCEIJX-PNKAXBHOSA-N
SMILESN([C@H]1[C@H](O[C@@H]([C@@H]([C@@H]1O)O)C)O[C@H]2[C@@H](C=C5C2CC#C[C@H]6O[C@]6(C#C5)[C@@H]7OC(=O)OC7)OC(=O)c3c4c(c(cc(c4)OC)C)ccc3O)C
安全數(shù)據(jù)
存儲(chǔ)類別10 - Combustible liquids
毒性LD50 in mice (mg/kg): 1050 orally, 0.96 i.v. (Toriyama)
常見問題列表
簡介
新制癌菌素(簡稱 NCS)是 1 種臨床抗癌抗生素，由制癌鏈霉菌（Streptomyces carzinostaticus）產(chǎn)生，它是雙烯二炔類抗癌抗生素色蛋白家族中的一員，由非蛋白生色團(tuán)(NCS-C)和載體蛋白(Apo-NCS)組成。它的抗腫瘤功能源于蛋白質(zhì)釋放的生色團(tuán)。生物活性
Neocarzinostatin 是一種有效的 DNA 損傷的、抗腫瘤抗生素，可識(shí)別雙鏈 DNA 膨脹并誘導(dǎo)DNA雙鏈斷裂 (DSBs)。Neocarzinostatin 誘導(dǎo)細(xì)胞凋亡 (apoptosis)。Neocarzinostatin 具有用于 EpCAM 陽性腫瘤的潛力。體外研究
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.