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Lapatinib (GW2016) is a potent inhibitor of the ErbB-2 and EGFR kinases at IC50 values of 10.2 and 9.8 nM. [1] In EGFR- and ErbB-2-overexpressing tumor cell lines such asA-431, HN5, BT474, N87, and CaLu-3, Lapatinibs growth inhbiition IC50 values were
Lapatinib treatment results in differential expression of genes associated with cell cycle regulation. These genes are mostly involved with the G1S phase transitions. [3]
Technical information:
| Chemical Formula: | C29H26ClFN4O4S | |
| CAS #: | 231277-92-2 | |
| Molecular Weight: | 581.06 | |
| Purity: | > 98% | |
| Appearance: | Light Yellow | |
| Chemical Name: | N-(4-(3-fluorobenzyloxy)-3-chlorophenyl)-6-(5-((2-(methylsulfonyl)ethylamino)methyl)furan-2-yl)quinazolin-4-amine,di4-methylbenzenesulfonate | |
| Solubility: | Up to 100mM in DMSO | |
| Synonyms: | GW572016, GW 572016, Tycerb, Tykerb, GSK 572016, Lapatinib |
Shipping Condition: The product is shipped in a glass vial at ambient temperature.
Storage condition: For longer shelf life, store solid powder at 4oC desiccated, or store DMSO solution at -20oC.
Reference:
| 1. | Rusnak et al., The effects of the novel, reversible epidermal growth factor receptor/ErbB-2 tyrosine kinase inhibitor, GW2016, on the growth of human normal and tumor-derived cell lines in vitro and in vivo. Mol. Cancer Ther. 2001, 1, 85-94. Pubmed ID: 12467226 |
| 2. | Hegde et al., Delineation of molecular mechanisms of sensitivity to lapatinib in breast cancer cell lines using global gene expression profiles. Mol. Cancer Ther. 2007, 6 1629-1640. Pubmed ID: 17513611 |