Lapatinib, EGFR and HER2 tyrosine kinase inhibitor (ab219408)

Overview

  • Product name

    Lapatinib, EGFR and HER2 tyrosine kinase inhibitor
  • Description

    Cell-permeable, potent EGFR and HER2 tyrosine kinase inhibitor
  • Alternative names

    • GSK572016
    • GW 572016
    • GW572016
    • Tyverb
  • Biological description

    Cell-permeable, potent dual tyrosine kinase inhibitor of EGFR and HER2 (ERBB2) (IC50 values are 3 nM and 13 nM respectively). Also inhibits HER4 (IC50 = 347 nM). Reduces tyrosine phosphorylation of EGFR and HER2, and inhibits activation of Erk1/2 and AKT, downstream effectors of proliferation and cell survival, respectively. Inhibits tumor cell growth in vitro and in xenograft models for a variety of human tumors. Effective in vivo and is used in combination therapy to prevent or suppress cancers where these kinases are over-expressed, including breast cancer.

  • Purity

    > 98%
  • CAS Number

    231277-92-2
  • Chemical structure

    Chemical Structure

Properties

  • Chemical name

    N-[3-Chloro-4-[(3-fluorophenyl)methoxy]phenyl]-6-[5-[(2-methylsulfonylethylamino)methyl]-2-furyl]quinazolin-4-amine
  • Molecular weight

    581.06
  • Molecular formula

    C29H26ClFN4O4S
  • PubChem identifier

    208908
  • Storage instructions

    Shipped at Room Temperature. Store at -20°C long term. Store under desiccating conditions.
  • Solubility overview

    Soluble in DMSO to 100 mM
  • Handling

    Wherever possible, you should prepare and use solutions on the same day. However, if you need to make up stock solutions in advance, we recommend that you store the solution as aliquots in tightly sealed vials at -20°C. Generally, these will be useable for up to one month. Before use, and prior to opening the vial we recommend that you allow your product to equilibrate to room temperature for at least 1 hour.

    Need more advice on solubility, usage and handling? Please visit our frequently asked questions (FAQ) page for more details.

  • SMILES

    CS(=O)(=O)CCNCC1=CC=C(O1)C2=CC3=C(C=C2)N=CN=C3NC4=CC(=C(C=C4)OCC5=CC(=CC=C5)F)Cl
  • Source

    Synthetic

References

This product has been referenced in:

  • Botrel TE  et al. Lapatinib plus chemotherapy or endocrine therapy (CET) versus CET alone in the treatment of HER-2-overexpressing locally advanced or metastatic breast cancer: systematic review and meta-analysis. Core Evid 8:69-78 (2013). Read more (PubMed: 24115917) »
  • Chu I  et al. The dual ErbB1/ErbB2 inhibitor, lapatinib (GW572016), cooperates with tamoxifen to inhibit both cell proliferation- and estrogen-dependent gene expression in antiestrogen-resistant breast cancer. Cancer Res 65:18-25 (2005). Read more (PubMed: 15665275) »
  • Burris HA Dual kinase inhibition in the treatment of breast cancer: initial experience with the EGFR/ErbB-2 inhibitor lapatinib. Oncologist 9 Suppl 3:10-5 (2004). Read more (PubMed: 15163842) »
  • Wood ER  et al. A unique structure for epidermal growth factor receptor bound to GW572016 (Lapatinib): relationships among protein conformation, inhibitor off-rate, and receptor activity in tumor cells. Cancer Res 64:6652-9 (2004). Read more (PubMed: 15374980) »
  • Xia W  et al. Anti-tumor activity of GW572016: a dual tyrosine kinase inhibitor blocks EGF activation of EGFR/erbB2 and downstream Erk1/2 and AKT pathways. Oncogene 21:6255-63 (2002). Read more (PubMed: 12214266) »

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Please note: All products are "FOR RESEARCH USE ONLY. NOT FOR USE IN DIAGNOSTIC PROCEDURES, NOT FOR USE IN HUMANS"
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