Afatinib-d6

Afatinib-d6 is intended for use as an internal standard for the quantification of afatinib (Cay-21567, Cay-11492) by GC- or LC-MS. 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: (2E)-N-[4-[(3-chloro-4-fluorophenyl)amino]-7-[[(3S)-tetrahydro-3-furanyl]oxy]-6-quinazolinyl]-4-[di(methyl-d3)amino]-2-butenamide. CAS Number: 1313874-96-2. Molecular Formula: C24H19ClD6FN5O3. Formula Weight: 492.0. Purity: >99% deuterated forms (d1-d6). Formulation: (Request formulation change), A solid. Solubility: DMF: 30 mg/ml, DMSO: 30 mg/ml, Ethanol: 30 mg/ml. lambdamax: 254, 343 nm. SMILES: FC(C=C1)=C(Cl)C=C1NC2=NC=NC3=C2C=C(NC(/C=C/CN(C([2H])([2H])[2H])C([2H])([2H])[2H])=O)C(O[C@@H]4COCC4)=C3. InChi Code: InChI=1S/C24H25ClFN5O3/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/h3-6,10-12,14,16H,7-9,13H2,1-2H3,(H,30,32)(H,27,28,29)/b4-3+/t16-/m0/s1/i1D3,2D3. InChi Key: ULXXDDBFHOBEHA-VCXSEIMGSA-N.