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Lapatinib ditosylate

Chemical Structure : Lapatinib ditosylate

CAS No.: 388082-77-7

Lapatinib ditosylate (GW 572016 ditosylate;GW-572016 ditosylate)

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.

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Purity & Documentation Purity: >98% (HPLC) Select Batch:

Biological Activity

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.

Physicochemical Properties

M.Wt 925.4608
Formula C43H42ClFN4O10S3
Appearance Solid
CAS No.
Storage
Solide Powder
-20 °C 12 Months; 4°C 6 Months
In Solvent
-80 °C 6 Months; -20°C 6 Months
Shipping
Solubility

10 mM in DMSO

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)

References

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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