Lapatinib

Lapatinib is a dual inhibitor of the EGF receptor (EGFR) and ErbB2 (IC50s = 19 and 3 nM, respectively). It inhibits the growth of EGFR-overexpressing A431 skin cancer and ErbB2-overexpressing SK-BR-3 breast cancer cells (IC50s = 0.14 and 0.124 µM, respectively). Lapatinib also inhibits the growth of ErbB2-amplified OD19 esophageal and NCI-N87 gastric cancer cells (IC50s = 0.09 and 0.01 µM, respectively) as well as several types of gastric cancer cells in which ErbB2 is not amplified (IC50s = 0.35-8.58 µM). It induces apoptosis in NCI-N87 and OD19 cells when used at a concentration of 1 µM. Lapatinib (50 mg/kg) reduces tumor growth in a BT474 breast cancer mouse xenograft model. It also reduces tumor growth in an NCI-N87 mouse xenograft model when administered at a dose of 100 mg/kg and induces tumor regression when used in combination with trastuzumab. Formulations containing lapatinib have been used in combination with other therapeutics in the treatment of HER2-overexpressing breast cancer.Formal Name: N-[3-chloro-4-[(3-fluorophenyl)methoxy]phenyl]-6-[5-[[[2-(methylsulfonyl)ethyl]amino]methyl]-2-furanyl]-4-quinazolinamine. CAS Number: 231277-92-2. Synonyms: GSK 572016, GW 572016. Molecular Formula: C29H26ClFN4O4S. Formula Weight: 581.1. Purity: >98%. Formulation: (Request formulation change), A crystalline solid. Solubility: DMF: 20 mg/ml, DMSO: 20 mg/ml, DMSO:PBS(pH 7.2) (1:2): 0.33 mg/ml. lambdamax: 245, 262, 306, 332, 362 nm. SMILES: O=S(CCNCC(O1)=CC=C1C2=CC3=C(N=CN=C3NC4=CC=C(OCC5=CC(F)=CC=C5)C(Cl)=C4)C=C2)(C)=O. InChi Code: InChI=1S/C29H26ClFN4O4S/c1-40(36,37)12-11-32-16-23-7-10-27(39-23)20-5-8-26-24(14-20)29(34-18-33-26)35-22-6-9-28(25(30)15-22)38-17-19-3-2-4-21(31)13-19/h2-10,13-15,18,32H,11-12,16-17H2,1H3,(H,33,34,35). InChi Key: BCFGMOOMADDAQU-UHFFFAOYSA-N.