| 9-amino Camptothecintopoisomerase I inhibitor |
Sample solution is provided at 25 µL, 10mM.
Nature.2017 Jan 19;541(7637):417-420.
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Chemical structure
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| Cas No. | 91421-43-1 | SDF | Download SDF |
| Synonyms | NSC 603071 | ||
| Chemical Name | (4S)-10-amino-4-ethyl-4-hydroxy-1H-pyrano[3",4":6,7]indolizino[1,2-b]quinoline-3,14(4H,12H)-dione | ||
| Canonical SMILES | O=C([C@@]1(CC)O)OCC2=C1C=C(C(N=C(C=CC=C3N)C3=C4)=C4C5)N5C2=O | ||
| Formula | C20H17N3O4 | M.Wt | 363.4 |
| Solubility | ≤1mg/ml in DMSO;1mg/ml in dimethyl formamide | Storage | Store at -20°C |
| Physical Appearance | A crystalline solid | Shipping Condition | Evaluation sample solution : ship with blue ice.All other available size:ship with RT , or blue ice upon request |
| General tips | For obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while.Stock solution can be stored below -20℃ for several months. | ||
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].
References:[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.
