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    Lapatinib Ditosylate (GW-572016, Tykerb)
    Lapatinib Ditosylate (GW-572016, Tykerb)

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    This product is for research use only, not for human use. We do not sell to patients.
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    InvivoChem Cat #: V0535
    CAS #: 388082-77-7 Purity ≥98%

    Description: Lapatinib Ditosylate  (formerly GW-572016, GW572016; trade names Tykerb and Tyverb) is an orally bioavailable medication acting as an EGFR (epidermal growth factor receptor) and ErbB2 inhibitor with antineoplastic activity. It inhibits EGFR and ErbB2 with IC50s of 10.8 and 9.2 nM in cell-free assays, respectively. It is an FDA approved drug for treating breast cancer and other solid tumors. 

    References: Mol Cancer Ther. 2001 Dec;1(2):85-94; Cancer Res. 2006 Feb 1;66(3):1630-9.

    Related CAS: 231277-92-2 (free base); 388082-77-7 (ditosylate) 

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    Molecular Weight (MW)925.46
    FormulaC29H26ClFN4O4S.2C7H8O3S
    CAS No.388082-77-7 (Lapatinib Ditosylate); 
    Storage-20℃ for 3 years in powder form
    -80℃ for 2 years in solvent
    Solubility (In vitro)DMSO: 100 mg/mL (108.1 mM)
    Water: <1 mg/mL
    Ethanol: <1 mg/mL
    Solubility (In vivo)2% DMSO+30% PEG 300+ddH2O: 10 mg/mL
    SynonymsGSK 572016; Trade name: Tykerb.GW2016; GSK 572016 ditosylate; GW-2016 ditosylate; GSK-572016 ditosylate; GSK-572016; GW-2016; GSK572016 ditosylate; GW2016 ditosylate; GW 2016; Lapatinib ditosylate; SK572016; GW 2016; Lapatinib;  

    Chemical Name: N-(3-chloro-4-((3-fluorobenzyl)oxy)phenyl)-6-(5-(((2-(methylsulfonyl)ethyl)amino)methyl)furan-2-yl)quinazolin-4-amine ditosylate

    InChi Key: UWYXLGUQQFPJRI-UHFFFAOYSA-N

    InChi Code: InChI=1S/C29H26ClFN4O4S.2C7H8O3S/c1-40(36,37)12-11-32-16-23-7-10-27(39-23)20-5-8-26-24(14-20)29(34-18-33-26)35-22-6-9-28(25(30)15-22)38-17-19-3-2-4-21(31)13-19;2*1-6-2-4-7(5-3-6)11(8,9)10/h2-10,13-15,18,32H,11-12,16-17H2,1H3,(H,33,34,35);2*2-5H,1H3,(H,8,9,10)

    SMILES Code: O=S(CCNCC1=CC=C(C2=CC3=C(NC4=CC=C(OCC5=CC=CC(F)=C5)C(Cl)=C4)N=CN=C3C=C2)O1)(C)=O.OS(=O)(C6=CC=C(C)C=C6)=O.OS(=O)(C7=CC=C(C)C=C7)=O


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    In Vitro

    In vitro activity: Lapatinib Ditosylate weakly inhibits the activity of ErbB4 with IC50 of 367 nM, and displays >300-fold selectivity for EGFR and ErbB2 over other kinases such as c-Src, c-Raf, MEK, ERK, c-Fms, CDK1, CDK2, p38, Tie-2, and VEGFR2. Lapatinib Ditosylate significantly inhibits receptor autophosphorylation of EGFR and ErbB2 in a dose-dependent manner with IC50 of 170 nM and 80 nM, respectively in HN5 cells; as well as 210 nM and 60 nM, respectively in BT474 cells. Unlike OSI-774 and Iressa (ZD1839) which preferentially inhibit the growth of the EGFR-overexpressing cells, Lapatinib Ditosylate inhibits the growth of both EGFR- and ErbB2-overexpressing cells. Lapatinib Ditosylate displays higher inhibitory activity against EGFR- or ErbB2-overexpressing cells with IC50 of 0.09-0.21 μM, compared with cells expressing low levels of EGFR or ErbB2 with IC50 of 3-12 μM, and exhibits ~100-fold selectivity over the normal fibroblast cells. Lapatinib Ditosylate potently inhibits the outgrowth of EGFR-overexpressing HN5 and A-431 cells, as well as ErbB2-overexpressing BT474 and N87 cells, and significantly induces G1 arrest of HN5 cells and apoptosis of BT474 cells, which are associated with inhibition of AKT phosphorylation.


    Kinase Assay: The IC50 values for inhibition of enzyme activity are generated by measuring inhibition of phosphorylation of a peptide substrate. The intracellular kinase domains of EGFR and ErbB2 are purified from a baculovirus expression system. EGFR and ErbB2 reactions are performed in 96-well polystyrene round-bottomed plates in a final volume of 45 μL. Reaction mixtures contain 50 mM 4-morpholinepropanesulfonic acid (pH 7.5), 2 mM MnCl2, 10 μM ATP, 1 μCi of [γ33P] ATP/reaction, 50 μM Peptide A [Biotin-(amino hexonoic acid)-EEEEYFELVAKKK-CONH2], 1 mM dithiothreitol, and 1 μL of DMSO containing serial dilutions of Lapatinib beginning at 10 μM. The reaction is initiated by adding the indicated purified type-1 receptor intracellular domain. The amount of enzyme added is 1 pmol/reaction (20 nM). Reactions are terminated after 10 minutes at 23°C by adding 45 μL of 0.5% phosphoric acid in water. The terminated reaction mix (75 μL) is transferred to phosphocellulose filter plates. The plates are filtered and washed three times with 200 μL of 0.5% phosphoric acid. Scintillation cocktail (50 μL) is added to each well, and the assay is quantified by counting in a Packard Topcount. IC50 values are generated from 10-point dose-response curves. 


    Cell Assay: Cells are exposed to various concentrations of Lapatinib for 72 hours. Relative cell number is estimated using methylene blue staining. The absorbance at 620 nm is read in a Spectra microplate reader. Cell death and cell cycle analysis are assessed by propidium iodide staining and antibody detection of incorporated BrdUrd and staining with propidium iodide.

    In VivoOral administration of Lapatinib Ditosylate (~100 mg/kg) twice daily significantly inhibits the growth of BT474 and HN5 xenografts in a dose-dependent manner.
    Animal modelCD-1 nude female mice implanted s.c. with HN5 cells, and C.B-17 SCID female mice implanted s.c. with BT474 cells
    Formulation & Dosage Dissolved in a vehicle of sulfo-butyl-ether-β-cyclodextrin 10% aqueous solution (CD10); 100 mg/kg; Oral gavage
    References

    Mol Cancer Ther. 2001 Dec;1(2):85-94; Cancer Res. 2006 Feb 1;66(3):1630-9.


    These protocols are for reference only. InvivoChem does not independently validate these methods.

    Lapatinib Ditosylate

    Lapatinib Ditosylate


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