91421-43-1
91421-43-1 结构式
基本信息
(20S)-9-氨基喜树碱
9-Amino-20-(S)-camptothecin
9-AMINO-CAMPTOTHECIN
CAMPTOTHECIN, 9-AMINO-
(20S)-9-AMINOCAMPTOTHECIN
9-Aminocamptothecin，9-Amino-20-(S)-camptothecin
(4S)-4α-Ethyl-4,12-dihydro-4-hydroxy-10-amino-1H-pyrano[3',4':6,7]indolizino[1,2-b]quinoline-3,14-dione
9-Amino-20(S)-camptothecine
NSC-603071
物理化学性质
常见问题列表
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Topo I
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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.
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.