Title: Lapatinib
CAS Registry Number: 231277-92-2
CAS Name: N-[3-Chloro-4-[(3-fluorophenyl)methoxy]phenyl]-6-[5[[[2-(methylsulfonyl)ethyl]amino]methyl]-2-furanyl]-4-quinazolinamine
Manufacturers' Codes: GW-572016
Trademarks: Tykerb (GSK)
Molecular Formula: C29H26ClFN4O4S
Molecular Weight: 581.06
Percent Composition: C 59.94%, H 4.51%, Cl 6.10%, F 3.27%, N 9.64%, O 11.01%, S 5.52%
Literature References: Reversible dual inhibitor of ErbB1 and ErbB2 tyrosine kinases. Prepn: M. C. Carter et al., WO 9935146 (1999 to Glaxo); eidem, US 6727256 (2004 to SmithKline Beecham). Mechanism of action study: W. Xia et al., Oncogene 21, 6255 (2002); and crystal structure in complex with epidermal growth factor receptor (EGFR, ErbB1): E. R. Wood et al., Cancer Res. 64, 6652 (2004). In vitro antitumor activity in combination with anti-ErbB2 antibodies: W. Xia et al., Oncogene 24, 6213 (2005). Biologic effects on tumor growth: N. L. Spector et al., J. Clin. Oncol. 23, 2502 (2005). Pharmacokinetics and clinical activity in metastatic carcinomas: H. A. Burris III et al., ibid. 5305. Review of clinical development: T. E. Kim, J. R. Murren, IDrugs 6, 886-893 (2003); H. A. Burris III, Oncologist 9, Suppl. 3, 10-15 (2004).
Derivative Type: Ditoluenesulfonate monohydrate
CAS Registry Number: 388082-78-8; 388082-77-7 (anhydrous)
Additional Names: Lapatinib ditosylate
Manufacturers' Codes: GW-572016F
Molecular Formula: C29H26ClFN4O4S.2C7H8O3S.H2O
Molecular Weight: 943.48
Percent Composition: C 54.74%, H 4.70%, Cl 3.76%, F 2.01%, N 5.94%, O 18.65%, S 10.20%
Properties: Yellow solid.
Therap-Cat: Antineoplastic.
Keywords: Antineoplastic; Tyrosine Kinase Inhibitors. |