- 英文名称
- 9-Aminocamptothecin
- 分子式
- C20H17N3O4
- 分子量
- 363.37
- 中文别名
- (S)-10-氨基-4-乙基-4-羟基-1H-吡喃并[3',4':6,7]吲哚并[1-2,b]喹啉-3,14(4H,12H)-二酮; (20S)-9-氨基喜树碱; 9-amino-CPT; 4':6,7)indolizino(1,2-B)quinoline-3,14(4H,12H)-dione; 4':6,7)indolizino(1,2-B)quinoline-3,14(4H,12H)-dione, 10-amino-4-ethyl-4-hydroxy-, (S)-; CAMPTOTHECIN, 9-AMINO-(RG); (S)-10-AMino-4-ethyl-4-hydroxy-1H-pyrano[3',4':6,7]indolizino[1,2-b]quinoline-3,14(4H,12H)-dione; (S)-10-Amino-4-ethyl-4-hydroxy-1H-pyrano[3',4':6,7]-indolizino[1,2-b]quinoline-3,14(4H,12H)-di; CAMPTOTHECIN, 9-AMINO-; AMinocaMptothecin; 9-AMINO-CAMPTOTHECIN; Camptothecin,9-amino; 9-Amino-20-camptothecin; 9-AC; 9-AMINO-20(S)-CAMPTOTHECIN; (20S)-9-aminocamptothecin; (4S)-10-Amino-4-ethyl-4-hydroxy-1H-pyrano[3',4':6,7]indolizino[1,2-b]quinoline-3,14(4H,12H)-dione
- 用途
- - 生物活性
9-amino-CPT (9-Aminocamptothecin, 9-AC, Aminocamptothecin, 9-amino-20(S)-camptothecin)是一种 Topoisomerase I 抑制剂并具有有效的抗癌活性。9-amino-CPT (9-Aminocamptothecin) 是喜树碱的一种具有活性的、不溶于水的衍生物。
- 靶点
Target
Value
Topo I
()
- 体外研究
In human breast (MCF-7), bladder (MGH-U1), and colon (HT-29) cancer cell lines, 9-Aminocamptothecin cytotoxicity increases with both higher drug concentrations and longer exposure times. Minimal cell killing is also observed unless 9-Aminocamptothecin concentrations exceeds a threshold of 2.7 nm. 9-Aminocamptothecin inhibits PC-3, PC-3M, DU145, and LNCaP cells with IC
50
values of 34.1, 10, 6.5, and 8.9 nM, respectively after 96 h of drug exposure.
- 体内研究
9-amino-CPT (9-amino-20(S)-camptothecin) inhibits tumor growth at the lowest oral dose (0.35 mg/kg/day), whereas higher oral doses (0.75 and 1 mg/kg/day) and s.c. administration (4 mg/kg/week) causes tumor regression. 9-amino-CPT (9-amino-20(S)-camptothecin) is well tolerated at all doses, with no toxic death or weight loss of more than 10% observed in any group. 9-amino-CPT (9-amino-20(S)-camptothecin) induces complete remissions in 55 % of SCID mice engrafted with human myeloid leukemia. The oral and intravenous routes are equally effective. The results with this pre-clinical model support the evaluation of 9-Aminocamptothecin as antileukemic agent in a phase I trial in patients with AML.
- 化学性质
黄色结晶粉末，可溶于甲醇、乙醇、DMSO等有机溶剂，来源于珙桐科植物喜树Camptotheca acuminata Decne.的果实。
- 用于含量测定/鉴定/药理实验等。
药理药效:抗肿瘤
- 中药对照品
