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Render Timestamp: 2024-12-04T08:56:02.701Z
Commit: cd2fae6ca3f811b1ddb1df24ac291ed56d5d501b
XML generation date: 2024-09-20 06:14:17.353
Product last modified at: 2024-09-19T22:13:05.750Z
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PDP - Template Name: Chemical Modulators
PDP - Template ID: *******c501c72

Lapatinib #12121

    Product Information

    Product Usage Information

    Lapatinib is supplied as a lyophilized powder. For a 10 mM stock, reconstitute the 10 mg in 1.08 ml DMSO. Working concentrations and length of treatment can vary depending on the desired effect, but is typically used at 0.1-10 µM either as a pretreatment for 0.5-2 hr prior to treating with a stimulator or used alone with varying treatment times lasting up to 72 hr.

    Storage

    Store lyophilized or in solution at -20ºC, desiccated. Protect from light. In lyophilized form, the chemical is stable for 24 months. Once in solution, use within 3 months to prevent loss of potency. Aliquot to avoid multiple freeze/thaw cycles.

    Product Description

    Molecular Weight 925.46 g/mol
    Purity >99%
    Molecular Formula C29H26ClFN4O4S•2C7H8O3S
    CAS 388082-77-7
    Solubility Soluble in DMSO at 200mg/ml.

    Background

    Lapatinib is a dual inhibitor of EGFR and HER2 tyrosine kinases (1-4). Researchers have shown that lapatinib inhibits purified EGFR and HER2 tyrosine kinase domains in cell-free kinase assays with IC50 values of 10.8 nM and 9.2 nM, respectively, and HER4 with an IC50 of 367 nM. Lapatinib was greater than 300-fold more selective for HER2 and EGFR than many other kinases, including c-src, MEK, Erk, and p38 in these assays (1). Studies have shown that lapatinib effectively inhibits both EGFR and HER2 autophosphorylation in cell types over expressing these kinases, and cell growth inhibition is correlated with HER2 overexpression (2-4).
    For Research Use Only. Not For Use In Diagnostic Procedures.
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