9-amino Camptothecin

- Overview
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    Background
    
    9-amino Camptothecin is a topoisomerase I inhibitor [1][2].
    DNA topoisomerases relax DNA torsional strain generated during replication, transcription, recombination, repair, and chromosome condensation. The relaxation of DNA supercoiling by topoisomerase I is enabled by a mechanism of controlled rotation around a transient DNA single-strand break. Camptothecin (CPT) is isolated from the bark of the Chinese tree Camptotheca accuminata [3].
    9-amino Camptothecin, a water-soluble camptothecin analogue, is a topoisomerase I inhibitor. In human HT-29 colon adenocarcinoma, 9-amino Camptothecin (9-AC) exhibited cytotoxicity with IC50 value of 19 nM. 9-AC also induced DNA damage in whole cells and nuclei at a concenstration of 85 nM and 21 nM, respectively [1].
    9-amino Camptothecin had greater activity than camptothecin against human tumour xenografts, including Lewis lung carcinoma and B16 melanoma. 9-AC had entered phase II trials. In patients with advanced solid tumours, 9-amino Camptothecin exhibited anti-tumor activity [1][2].
    
    [1]. Rothenberg, M.L. Topoisomerase I inhibitors: Review and update. Annals of Oncology 8(9), 837-855 (1997).
    [2]. Dancey J, Eisenhauer EA. Current perspectives on camptothecins in cancer treatment. Br J Cancer. 1996 Aug;74(3):327-38.
    [3]. Drwal MN1, Agama K, Wakelin LP, et al. Exploring DNA topoisomerase I ligand space in search of novel anticancer agents. PLoS One. 2011;6(9):e25150.
- Properties
  - Alternative Name
    
    NSC 603071; (4S)-10-amino-4-ethyl-4-hydroxy-1H-pyrano[3',4':6,7]indolizino[1,2-b]quinoline-3,14(4H,12H)-dione
    
    CAS Number
    
    91421-43-1
    
    Molecular Formula
    
    C20H17N3O4
    
    Molecular Weight
    
    363.4
    
    Appearance
    
    A crystalline solid
    
    Purity
    
    Purity ≥ 95.00%
    
    Solubility
    
    ≤1mg/ml in DMSO;1mg/ml in dimethyl formamide
    
    Storage
    
    Store at -20°C
    
    * For Research Use Only

9-amino Camptothecin

Background

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