Lapatinib Tosylate

Cat. No. IC23176

CAS. No. 1187538-35-7

Key Features and Details

Category

Inhibitor&Activator

Formula

C36H34ClFN4O7S2

Product Size

Online Inquiry

Product Details

Product Name

Lapatinib Tosylate

CAS No.

1187538-35-7

Molecular Weight

753.26

Synonyms

GW572016 tosylate; GW2016 tosylate

Formula

C36H34ClFN4O7S2

SMILES

O=S(C1=CC=C(C)C=C1)(O)=O.O=S(CCNCC2=CC=C(C3=CC=C4C(C(NC5=CC(Cl)=C(C=C5)OCC6=CC(F)=CC=C6)=NC=N4)=C3)O2)(C)=O

Product Overview

Description

Lapatinib (GW572016) tosylate is a potent, orally active inhibitor of the ErbB-2 and EGFR tyrosine kinase domains with IC50 values against purified EGFR and ErbB-2 of 10.2 and 9.8 nM, respectively.

In Vitro Activity

Lapatinib (GW2016; 0.03-10 µM; 6 hours; BT474 and HN5 cells) tosylate treatment inhibits receptor autophosphorylation of EGFR and ErbB-2 in a dose-responsive manner. Phosphorylation of serine 473 of AKT was inhibited by GW2016 in a dose-dependent manner. Lapatinib (GW2016; 72 hours; HN5, A-43, BT474, N87, and CaLu-3 cells) tosylate treatment has a selective inhibition of the proliferation of human tumor cell lines. Lapatinib (GW2016; 1-10 µM; 72 hours; HN5 cells) treatment results in induces G1 arrest.

In Vivo Activity

Lapatinib (GW2016; 30-100 mg/kg; oral administration; twice daily; for 21 days; CD-1 nude female mice) tosylate treatment inhibits tumor xenograft growth of the HN5 cells in a dose-responsive manner at 30 and 100 mg/kg, with complete inhibition of tumor growth at the higher dose.

Storage & Handling

Storage

Please store the product under the recommended conditions in the Certificate of Analysis.

Shipping

Room temperature in continental US; may vary elsewhere.

All of our services and products are intended for preclinical research use only and cannot be used to diagnose, treat or manage patients.