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Submit ReviewLapatinib 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.
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.
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.
Solvent | Max Conc. mg/mL | Max Conc. mM | |
---|---|---|---|
Solubility | |||
DMSO | 58.11 | 100 |
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 |
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.
Keywords: Lapatinib, Lapatinib supplier, Potent, selective, dual, ErbB2, (HER-2), and, EGFR, inhibitors, inhibits, 6811, Tocris Bioscience
Citations are publications that use Tocris products.
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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.
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.