9-amino-CPT 是一种拓扑异构酶I的抑制剂,具有抗肿瘤活性。
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9-Aminocamptothecin is an inhibitor of topoisomerase I with potent anticancer activity.
体外活性
9-Aminocamptothecin inhibits PC-3, PC-3M, DU145, and LNCaP cells with IC50 values of 34.1, 10, 6.5, and 8.9 nM, respectively after 96 h of drug exposure [1]. In human bladder (MGH-U1), breast (MCF-7), 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 exceed a threshold of 2.7 nM [2].
体内活性
9-Aminocamptothecin 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 [1]. 9-Aminocamptothecin induces complete remissions in 55 % of SCID mice engrafted with human myeloid leukemia. The oral and intravenous routes are equally effective [3].
Cas No.
91421-43-1
分子式
C20H17N3O4
分子量
363.4
别名
9-Aminocamptothecin;9-氨基喜树碱;Aminocamptothecin;9-amino-2(S)-camptothecin
储存和溶解度
DMSO:3.33 mg/mL (9.16 mM)
Powder: -20°C for 3 years
In solvent: -80°C for 2 years