Lapatinib (ditosylate) | CAS:388082-77-7

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Name:Lapatinib ditosylate; GW-572016 ditosylate
Cat. No. :CS-0831
CAS No. :388082-77-7
Formula:C43H42ClFN4O10S3
M. Wt. : 925.46
Solubility:DMSO: ≥150 mg/mL

Lapatinib ditosylate is a potent EGFR and ErbB2 inhibitor with IC50 of 10.2 and 9.8 nM, respectively. IC50 & Target: IC50: 10.2 nM (EGFR), 9.8 nM (ErbB2)[1]In Vitro: The IC50 of Lapatinib (GW2016) values for inhibition of enzyme activity are generated by measuring inhibition of phosphorylation of a peptide substrate. With the exception of ErbB-4 (IC50, 367 nM), Lapatinib is >300-fold selective for EGFR and ErbB-2 over other kinases tested[1]. IC50 values of Lapatinib (GW2016) for BT474, SKBR3, EFM192A, HCC1954, MDAMB453 and MDAMB231 cells is 36±15.1 nM, 80±17.3 nM, 193±66.5 nM, 416.6±180 nM, 6.08±0.825 μM and 7.46±0.102 μM, respectively. Treatment with Lapatinib results in IC50 values of ≤ 0.16 μM on the EGFR- and the ErbB-2-overexpressing tumor cell lines[2].In Vivo: Lapatinib (GW2016) is potent at inhibiting the growth of BT474 and HN5 human tumor xenografts. A dose-responsive inhibition of both models occurred on treatment of tumor-bearing mice with 30 and 100 mg/kg Lapatinib orally, twice daily. Complete inhibition of tumor growth is seen at the 100 mg/kg dose. At this dose, there is [1]. Lapatinib (100 mg/kg/day, oral gavage) induces severe oxidative damage in the cardiac tissue of rat[3].

Eryilmaz U, et al. S100A1 as a Potential Diagnostic Biomarker for Assessing Cardiotoxicity and Implications for the Chemotherapy of Certain Cancers. PLoS One. 2015 Dec 18;10(12):e0145418. Rusnak DW, 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 Dec;1(2):85-94. O'Neill F, et al. Gene expression changes as markers of early lapatinib response in a panel of breast cancer cell lines. Mol Cancer. 2012 Jun 18;11(1):41.