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- 9-amino Camptothecin
9-amino Camptothecin
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.
Physical Appearance | A crystalline solid |
Storage | Store at -20°C |
M.Wt | 363.4 |
Cas No. | 91421-43-1 |
Formula | C20H17N3O4 |
Synonyms | NSC 603071 |
Solubility | ≤1mg/ml in DMSO;1mg/ml in dimethyl formamide |
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 |
SDF | Download SDF |
Canonical SMILES | O=C([C@@]1(CC)O)OCC2=C1C=C(C(N=C(C=CC=C3N)C3=C4)=C4C5)N5C2=O |
Shipping Condition | Small Molecules with Blue Ice, Modified Nucleotides with Dry Ice. |
General tips | We do not recommend long-term storage for the solution, please use it up soon. |
Quality Control & MSDS
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Purity ≥ 95.00%
- COA (Certificate Of Analysis)
- MSDS (Material Safety Data Sheet)