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BC164610
BIO-X

Lapatinib base

Inhibitor of EGFR (ErbB1) and HER2 (ErbB2) receptor tyrosine kinases. Used for sensitization of HER2-overexpressing cancer cells to radiation as well as chemotherapy to tamoxifen- and trastuzumab-resistant cell lines. The compound blocks signalling via Akt and mitogen-activated protein kinase (MAPK) pathways leading to reduced cell survival. In trastuzumab resistant cancer cells, it inhibits HER2 phosphorylation, prevents receptor ubiquitination and causes accumulation of inactive HER2 dimers on the cell surface. 

Technical Data

CAS No: 231277-92-2
Synonyms: GW572016
Product Code: BC164610
MDL No: MFCD09264194
Chemical Formula: C29H26ClFN4O4S
Molecular Weight: 581.06

References


  • Nahta et al., 2007. Lapatinib induces apoptosis in trastuzumab-resistant breast cancer cells: effects on insulin-like growth factor I signalling. Mol Cancer Ther 6(2):667-74.
  • Scaltriti et al., 2009. Lapatinib, a HER2 tyrosine kinase inhibitor, induces stabilization and accumulation of HER2 and potentiates trastuzumab-dependent cell cytotoxicity. Oncogene 28(6):803-14.

Solubility

Stability

Further Information


Datasheets


CAS No:
231277-92-2
Synonyms:
GW572016
MDL No:
MFCD09264194
Chemical Formula:
Molecular Weight:
581.06
Product Structure
References:
1. Nahta et al., 2007. Lapatinib induces apoptosis in trastuzumab-resistant breast cancer cells: effects on insulin-like growth factor I signalling. Mol Cancer Ther 6(2):667-74.
2. Scaltriti et al., 2009. Lapatinib, a HER2 tyrosine kinase inhibitor, induces stabilization and accumulation of HER2 and potentiates trastuzumab-dependent cell cytotoxicity. Oncogene 28(6):803-14.

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