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Submit ReviewLapatinib
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)
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.
| 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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Product Datasheets for Lapatinib
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.
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Keywords: Lapatinib, Lapatinib supplier, Potent, selective, dual, ErbB2, (HER-2), and, EGFR, inhibitors, inhibits, 6811, Tocris Bioscience
Citations 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.
Cancer Research Product Guide
A collection of over 750 products for cancer research, the guide includes research tools for the study of:
- Cancer Metabolism
- Epigenetics in Cancer
- Receptor Signaling
- Cell Cycle and DNA Damage Repair
- Angiogenesis
- Invasion and Metastasis
Kinases Product Listing
A collection of over 400 products for kinase research, the listing includes inhibitors of:
- Receptor Tyrosine Kinases
- Protein Kinases A, C, D and G
- PI-3 Kinase, Akt and mTOR
- MAPK Signaling
- Receptor Serine/Threonine Kinases
Angiogenesis in Cancer Poster
Adapted from the 2015 Cancer Product Guide, Edition 3, this poster summarizes the pathogenesis of angiogenesis in cancer, as well as some of the main angiogenesis therapeutic targets.
Schizophrenia Poster
Schizophrenia is a debilitating psychiatric disorder that affects 1% of the worldwide population. This poster describes the neurobiology of Schizophrenia, as well as highlighting the genetic and environmental factors that play a fundamental role in the etiology of the disease. The current and emerging drug targets are also discussed.