Lapatinib

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Description: Potent and selective dual ErbB2 (HER-2) and EGFR inhibitor
Chemical Name: N-[3-Chloro-4-[(3-fluorophenyl)methoxy]phenyl]-6-[5-[[[2-(methylsulfonyl)ethyl]amino]methyl]-2-furanyl]-4-quinazolinamine
Purity: ≥98% (HPLC)
Datasheet
Citations (1)
Reviews
Literature (1)

Biological Activity for Lapatinib

Lapatinib is a potent and selective dual ErbB2 (HER-2) and EGFR inhibitor (IC50 values are 9.8 and 10.2 nM, respectively). Selective for EGFR and ErbB-2 versus other proliferative kinases. Inhibits proliferation in multiple cancer cell lines (average IC50 values <0.16 μM). Exhibits 100-fold average selectivity for the tumor cells versus human foreskin fibroblasts. Inhibits EGFR/ErbB2 autophosphorylation and phosphorylation of the downstream modulator AKT.

Compound Libraries for Lapatinib

Lapatinib is also offered as part of the Tocriscreen Kinase Inhibitor Library and Tocriscreen FDA-Approved Drugs. Find out more about compound libraries available from Tocris.

Technical Data for Lapatinib

M. Wt 581.06
Formula C29H26ClFN4O4S
Storage Store at -20°C
Purity ≥98% (HPLC)
CAS Number 231277-92-2
PubChem ID 208908
InChI Key BCFGMOOMADDAQU-UHFFFAOYSA-N
Smiles CS(=O)(CCNCC1=CC=C(C2=CC=C3N=CN=C(C3=C2)NC4=CC(Cl)=C(C=C4)OCC5=CC(F)=CC=C5)O1)=O

The technical data provided above is for guidance only. For batch specific data refer to the Certificate of Analysis.

Tocris products are intended for laboratory research use only, unless stated otherwise.

Solubility Data for Lapatinib

Solvent Max Conc. mg/mL Max Conc. mM
Solubility
DMSO 58.11 100

Preparing Stock Solutions for Lapatinib

The following data is based on the product molecular weight 581.06. Batch specific molecular weights may vary from batch to batch due to the degree of hydration, which will affect the solvent volumes required to prepare stock solutions.

Select a batch to recalculate based on the batch molecular weight:
Concentration / Solvent Volume / Mass 1 mg 5 mg 10 mg
1 mM 1.72 mL 8.6 mL 17.21 mL
5 mM 0.34 mL 1.72 mL 3.44 mL
10 mM 0.17 mL 0.86 mL 1.72 mL
50 mM 0.03 mL 0.17 mL 0.34 mL

Molarity Calculator

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Reconstitution Calculator

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Dilution Calculator

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Product Datasheets for Lapatinib

Certificate of Analysis / Product Datasheet
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References for Lapatinib

References are publications that support the biological activity of the product.

Rusnak et al (2001) The effects of the novel, reversible epidermal growth factor receptor/ErbB-2 tyrosine kinase inhibitor, GW2016, on the growth of human normal and tumor-derived cell lines in vitro and in vivo. Mol.Cancer Ther. 1 85 PMID: 12467226


If you know of a relevant reference for Lapatinib, please let us know.

View Related Products by Product Action

View all EGFR Inhibitors

Keywords: Lapatinib, Lapatinib supplier, Potent, selective, dual, ErbB2, (HER-2), and, EGFR, inhibitors, inhibits, 6811, Tocris Bioscience

1 Citation for Lapatinib

Citations are publications that use Tocris products. Selected citations for Lapatinib include:

Gregory et al (2021) A ligand-receptor interactome platform for discovery of pain mechanisms and therapeutic targets. Sci Signal 14 PMID: 33727337


Do you know of a great paper that uses Lapatinib from Tocris? Please let us know.

Reviews for Lapatinib

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Literature in this Area

Tocris offers the following scientific literature in this area to showcase our products. We invite you to request* your copy today!

*Please note that Tocris will only send literature to established scientific business / institute addresses.


Angiogenesis in Cancer Poster

Angiogenesis in Cancer Poster

This poster summarizes the pathogenesis of angiogenesis in cancer, as well as some of the main angiogenesis therapeutic targets.