Lapatinib (GW-572016)

InformationLapatinib (GW-572016, GSK572016, GW2016), used in the form of Lapatinib Ditosylate, is a potentEGFRandErbB2inhibitor withIC50of 10.8 and 9.2 nM in cell-free assays, respectively. Lapatinib inducesferroptosisandautophagic cell death.In vitroLapatinib 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 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 inhibits the growth of both EGFR- and ErbB2-overexpressing cells. Lapatinib 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 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.In vivoOral administration of Lapatinib (~100 mg/kg) twice daily significantly inhibits the growth of BT474 and HN5 xenografts in a dose-dependent manner.Cell Datacell lines：Concentrations：Dissolved in DMSO, final concentrations ~100 μMIncubation Time：72 hoursPowder Purity:≥99%. Specification: 10mM in DMSO Molecular Formula: C29H26ClFN4O4S Molecular Weight: 581.06

UPC:

51201539

Condition:

New

Weight:

0.85 Ounces

HazmatClass:

No

Quantity:

1

Unit of Measurement:

EA

WeightUOM:

LB

MPN:

L408018-1ml

CAS:

231277-92-2

Product Size:

1ml