Title: Exatecan
CAS Registry Number: 171335-80-1
CAS Name: (1S,9S)-1-Amino-9-ethyl-5-fluoro-1,2,3,9,12,15-hexahydro-9-hydroxy-4-methyl-10H,13H-benzo[de]pyrano[3¢,4¢:6,7]indolizino[1,2-b]quinoline-10,13-dione
Manufacturers' Codes: DX-8951
Molecular Formula: C24H22FN3O4
Molecular Weight: 435.45
Percent Composition: C 66.20%, H 5.09%, F 4.36%, N 9.65%, O 14.70%
Literature References: Topoisomerase I inhibitor; synthetic analogue of camptothecin, q.v. Prepn: H. Terasawa et al., EP 495432 (1992 to Daiichi); of mesylate: S. Kamihara et al., EP 737686; eidem, US 6552197 (1996, 2003 both to Daiichi). HPLC determn in mouse plasma: T. Oguma et al., Biol. Pharm. Bull. 24, 176 (2001). Clinical pharmacokinetics and evaluation in advanced leukemia: F. J. Giles et al., Clin. Cancer Res. 8, 2134 (2002); in advanced solid malignancies: M. A. Garrison et al., ibid. 9, 2527 (2003); in breast cancer: F. J. Esteva et al., Cancer 98, 900 (2003); in gastric cancer: J. A. Ajani et al., Invest. New Drugs 23, 479 (2005).
Derivative Type: Methanesulfonate dihydrate
CAS Registry Number: 197720-53-9; 169869-90-3 (anhydrous)
Additional Names: Exatecan mesylate
Manufacturers' Codes: DX-8951f
Molecular Formula: C24H22FN3O4.CH4O3S.2H2O
Molecular Weight: 567.58
Percent Composition: C 52.90%, H 5.33%, F 3.35%, N 7.40%, O 25.37%, S 5.65%
Properties: mp 245-255° (dec). Sol in water.
Melting point: mp 245-255° (dec)
Therap-Cat: Antineoplastic.
Keywords: Antineoplastic; Alkaloids/Natural Products; Camptothecin Derivatives; Topoisomerase I Inhibitor. |