Afatinib (maleate)

Afatinib is an irreversible inhibitor of epidermal growth factor receptor (EGFR) and ErbB2 (IC50s = 0.5 and 14 nM, respectively). It increases the cytotoxicity of adriamycin in a concentration-dependent manner in multidrug-resistant A549T lung cancer cells overexpressing P-glycoprotein. Afatinib (20 mg/kg) reduces tumor growth in ErbB2-amplified NCI-N87 and NUGC4 gastric cancer mouse xenograft models. Formulations containing afatinib have been used in the treatment of non-small cell lung cancer.Formal Name: N-[4-[(3-chloro-4-fluorophenyl)amino]-7-[[(3S)-tetrahydro-3-furanyl]oxy]-6-quinazolinyl]-4-(dimethylamino)-2E-butenamide, 2Z-butenedioate (1:2). CAS Number: 850140-73-7. Synonyms: Afatinib dimaleate, BIBW 2992, BIBW 2992MA2. Molecular Formula: C24H25ClFN5O3 . 2C4H4O4. Formula Weight: 718.1. Purity: >95%. Formulation: (Request formulation change), A crystalline solid. Solubility: DMF: 30 mg/mL, DMSO: 30 mg/mL, PBS (pH 7.2): 10 mg/mL. lambdamax: 253, 345 nm. SMILES: FC(C=C1)=C(Cl)C=C1NC2=NC=NC3=C2C=C(NC(/C=C/CN(C)C)=O)C(O[C@@H]4COCC4)=C3.OC(/C=C\C(O)=O)=O.OC(/C=C\C(O)=O)=O. InChi Code: InChI=1S/C24H25ClFN5O3.2C4H4O4/c1-31(2)8-3-4-23(32)30-21-11-17-20(12-22(21)34-16-7-9-33-13-16)27-14-28-24(17)29-15-5-6-19(26)18(25)10-15,2*5-3(6)1-2-4(7)8/h3-6,10-12,14,16H,7-9,13H2,1-2H3,(H,30,32)(H,27,28,29),2*1-2H,(H,5,6)(H,7,8)/b4-3+,2*2-1-/t16-,. InChi Key: USNRYVNRPYXCSP-JUGPPOIOSA-N.