| Description | 9-amino-CPT (Aminocamptothecin) is an inhibitor of topoisomerase I with potent anticancer activity. |
| In vitro | 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]. |
| In vivo | 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]. |
| Synonyms | 9-氨基喜树碱, Aminocamptothecin, 9-amino-2(S)-camptothecin, 9-Aminocamptothecin |
| molecular weight | 363.37 |
| Molecular formula | C20H17N3O4 |
| CAS | 91421-43-1 |
| Storage | Powder: -20°C for 3 years | In solvent: -80°C for 1 year |
| Solubility | DMSO: 3.33 mg/mL (9.16 mM) |
| References | 1. de Souza PL, et al. 9-Aminocamptothecin: a topoisomerase I inhibitor with preclinical activity in prostate cancer. Clin Cancer Res. 1997 Feb;3(2):287-94. 2. Li ML, et al. Pharmacological determinants of 9-aminocamptothecin cytotoxicity. Clin Cancer Res. 2001 Jan;7(1):168-74. 3. Jeha S, et al. Activity of oral and intravenous 9-aminocamptothecin in SCID mice engrafted with human leukemia. Leuk Lymphoma. 1998 Dec;32(1-2):159-64. |