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Cat.No. 6811 - Lapatinib | C29H26ClFN4O4S | CAS No. 231277-92-2
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)
Literature (4)

Biological Activity

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.

Technical Data

M. Wt 581.06
Formula C29H26ClFN4O4S
Storage Store at -20°C
Purity ≥98% (HPLC)
CAS Number 231277-92-2
PubChem ID 208908
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

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

Preparing Stock Solutions

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

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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.

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

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Literature in this Area

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