9-氨基喜树碱
中文名称:
9-氨基喜树碱
中文同义词:
9-氨基喜树碱;(S)-10-氨基-4-乙基-4-羟基-1H-吡喃并[3,4:6,7]1-吲哚啉嗪O[1,2-B]喹啉-3,14(4H,12H)-二酮;9-氨基喜树碱,(20S)-9-氨基喜树碱;9-AMINOCAMPTOTHECIN 9-氨基喜树碱;9-氨基喜树碱 250MG;(20S)-9-氨基喜树碱;9-氨基喜树碱, >96%;9-氨基喜树碱 标准品
英文名称:
9-Aminocamptothecin
英文同义词:
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
CAS号:
91421-43-1
分子式:
C20H17N3O4
分子量:
363.37
EINECS号:
相关类别:
化学连接;中药对照品;喜树碱系列;植物提取物;标准品;细胞生物学试剂;分析试剂标准品;Pharmaceutical Raw Materials;Alkaloids;Natural Anti-cancer Medical Materials and Its Derivatives;对照品-中药对照品;对照品;标准品 -中药标准品;医药原料药;医药、农药及染料中间体;标准品，对照品
Mol文件:
91421-43-1.mol
熔点
142.0-145.0 °C
沸点
819.6±65.0 °C(Predicted)
密度
1.55±0.1 g/cm3(Predicted)
储存条件
Keep in dark place,Sealed in dry,2-8°C
酸度系数(pKa)
11.23±0.20(Predicted)
Merck
14,431
InChIKey
FUXVKZWTXQUGMW-FQEVSTJZSA-N
CAS 数据库
91421-43-1(CAS DataBase Reference)
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
()
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。
用途
用于含量测定/鉴定/药理实验等。
药理药效:抗肿瘤
用途
中药对照品
RTECS号
UQ0490500
海关编码
29349990
