Formulation: A solid
Formal 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, monomethanesulfonate
Purity: ≥98%
Formula Markup: C24H22FN3O4 • CH3SO3H
CAS Number: 169869-90-3
Notes: Exatecan is a derivative of camptothecin (Item No. 11694) and DNA topoisomerase I inhibitor (IC50 = 0.975 µg/ml).{67022} It inhibits cell growth in a panel of 32 breast, colon, stomach, and lung cancer cell lines (GI50s = 0.125-10.4 ng/ml). Exatecan (3.325-50 mg/kg) reduces tumor growth in an SC-6-JCK gastric adenocarcinoma mouse xenograft model. It reduces tumor weight in HCT116, PC-6, and PC12 mouse xenograft models when administered at a dose of 75 mg/kg.{67023} Exatecan has also been used in the synthesis of cytotoxic payload moieties of antibody-drug conjugates (ADCs).{67024} Formulations containing exatecan have been used in the treatment of breast, gastric, and gastroesophageal cancers.