Lapatinib is an inhibitor of EGFR/HER2 (ErbB2) that is currently in clinical trials as a co-administered treatment with other chemotherapeutics. Lapatinib exhibits anticancer chemotherapeutic benefit, inducing apoptosis in breast cancer cells. This compound also downregulates expression of thymidylate synthase in vitro.
| Cas No. | 388082-78-8 |
|---|---|
| Purity | ≥98% |
| Formula | C26H26ClFN4O4S 2C7H8O3S H2O |
| Formula Wt. | 925.46 |
| IUPAC Name | N-[3-chloro-4-[(3-fluorophenyl)methoxy]phenyl]-6-[5-[(2-methylsulfonylethylamino)methyl]furan-2-yl]quinazolin-4-amine;4-methylbenzenesulfonic acid |
| Melting Point | 236-259°C |
| Solubility | Slightly in DMSO |
| Appearance | Pale yellow to yellow powder |
| Store Temp | 4°C |
|---|---|
| Ship Temp | Ambient |
| MSDS | L0360 MSDS PDF |
|---|---|
| Info Sheet | L0360 Info Sheet PDF |
Janni W, Sarosiek T, Karaszewska B, et al. A phase II, randomized, multicenter study evaluating the combination of lapatinib and vinorelbine in women with ErbB2 overexpressing metastatic breast cancer. Breast Cancer Res Treat. 2014 Jan 9. [Epub ahead of print]. PMID: 24402830.
Kostyal D, Welt RS, Danko J, et al. Trastuzumab and lapatinib modulation of HER2 tyrosine/threonine phosphorylation and cell signaling. Med Oncol. 2012 Sep;29(3):1486-94. PMID: 21769502.
Kim HP, Yoon YK, Kim JW, et al. Lapatinib, a dual EGFR and HER2 tyrosine kinase inhibitor, downregulates thymidylate synthase by inhibiting the nuclear translocation of EGFR and HER2. PLoS One. 2009 Jun 16;4(6):e5933. PMID: 19529774.
