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Chemical Structure : Lapatinib ditosylate
CAS No.: 388082-77-7
Catalog No.: PC-45895Not For Human Use, Lab Use Only.
Lapatinib (GW 572016) ditosylate is a reversible, selective dual tyrosine kinase inhibitor of both EGFR and ErbB2 with IC50 of 10.8 and 9.2 nM in cell-free assays, respectively.
| Packing | Price | Stock | Quantity |
|---|---|---|---|
| 50 mg (Free Sample) | $28 | In stock | |
| 100 mg | $78 | In stock | |
| 250 mg | $128 | In stock | |
| 1 g | Get quote |
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Lapatinib (GW 572016) ditosylate is a reversible, selective dual tyrosine kinase inhibitor of both EGFR and ErbB2 with IC50 of 10.8 and 9.2 nM in cell-free assays, respectively.
Lapatinib displays no significant activity against other kinases, including ErbB4, c-Src, and c-Raf1.
Lapatinib reduces tyrosine phosphorylation of EGFR and erbB2, and inhibits activation of Erk1/2 and AKT both in vitro and in vivo.
Lapatinib inhibits tumor xenograft growth of the HN5 and BT474 cells in a dose-responsive manner at 30 and 100 mg/kg; orally active.
| M.Wt | 925.4608 | |
| Formula | C43H42ClFN4O10S3 | |
| Appearance | Solid | |
| Storage |
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| Solubility |
10 mM in DMSO |
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| Chemical Name/SMILES |
4-Quinazolinamine, N-[3-chloro-4-[(3-fluorophenyl)methoxy]phenyl]-6-[5-[[[2-(methylsulfonyl)ethyl]amino]methyl]-2-furanyl]-, 4-methylbenzenesulfonate (1:2) |
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1. Xia W, et al. Oncogene. 2002 Sep 12;21(41):6255-63.
2. Rusnak DW, et al. Mol Cancer Ther. 2001 Dec;1(2):85-94.
3. Konecny GE, et al. Cancer Res. 2006 Feb 1;66(3):1630-9.
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