Lapatinib

Name: Lapatinib
Brand: Tocris Bioscience
SKU: 6811

Tocris Bioscience, part of Bio-Techne | Catalog # 6811

Citations (15)

COA / SDS

Potent and selective dual ErbB2 (HER-2) and EGFR inhibitor

Key Product Details

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)
Molecular Weight:	581.06

View Full Technical Details for Lapatinib

Technical Data
Citations

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 for Lapatinib

	Solvent	Max Conc. mg/mL	Max Conc. mM
Solubility
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.

Concentration / Solvent Volume / Mass	1 mg	5 mg	10 mg
1 mM	1.72 mL	8.60 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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Reconstitution Calculator

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References for Lapatinib

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

Rusnak 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. 2001 PMID: 12467226