Apaziquone, also known as EO9, EOquin, is a n indolequinone bioreductive prodrug and analog of mitomycin C with potential antineoplastic and radiosensitization activities. Apaziquone is converted to active metabolites in hypoxic cells by intracellular reductases, which are present in greater amounts in hypoxic tumor cells. The active metabolites alkylate DNA, resulting in apoptotic cell death. This agent displays activity towards both hypoxic solid tumors, which exhibits higher expression of cytochrome P450 reductase, and well-oxygenated malignant cells that overexpress the bioreductive enzyme NQO1 (NAD(P)H: quinone oxidoreductase). Apaziquone may selectively sensitize hypoxic tumor cells to radiocytotoxicity. Check for active clinical trials or closed clinical trials using this agent.
仅供研究使用。 我们不向患者出售。
化学信息
名称 | Apaziquone |
Iupac 化学名称 | 5-(aziridin-1-yl)-3-(hydroxymethyl)-2-[(E)-3-hydroxyprop-1-enyl]-1-methylindole-4,7-dione |
同义词 | EO9; NSC 382459 |
英文同义词 | EO9; NSC 382459 |
分子式 | C15H16N2O4 |
分子量 | 288.3 |
Smile | N1(CC1)C=1C(C=2C(=C(N(C2C(C1)=O)C)\C=C\CO)CO)=O |
InChiKey | MXPOCMVWFLDDLZ-NSCUHMNNSA-N |
InChi | InChI=1S/C15H16N2O4/c1-16-10(3-2-6-18)9(8-19)13-14(16)12(20)7-11(15(13)21)17-4-5-17/h2-3,7,18-19H,4-6,8H2,1H3/b3-2+ |
Cas号 | 114560-48-4 |
相关CAS号 | |
外观性状 | Solid powder |
纯度 | 98% by HPLC |
存储 | -20 ºC for 3 years |
可溶性 | Soluble in DMSO |
处理方式 | |
运输条件 | Shipped under ambient temperature |
海关编码 | |
Targets | |
Mechanism | |
Cell study | |
Animal study | |
Clinical study | |