Lapatinib Ditosylate

Cat. No. IC23154

CAS. No. 388082-77-7

Key Features and Details

Category

Inhibitor&Activator

Purity

99.95%

Formula

C43H42ClFN4O10S3

Product Size

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Product Details

Product Name

Lapatinib Ditosylate

CAS No.

388082-77-7

Molecular Weight

925.46

Synonyms

GW572016 ditosylate; GW2016 ditosylate

Formula

C43H42ClFN4O10S3

Appearance

Solid

Purity

99.95%

SMILES

O=S(CCNCC1=CC=C(C2=CC=C3C(C(NC4=CC(Cl)=C(C=C4)OCC5=CC(F)=CC=C5)=NC=N3)=C2)O1)(C)=O.O=S(C6=CC=C(C)C=C6)(O)=O.O=S(C7=CC=C(C)C=C7)(O)=O

Product Overview

Description

Lapatinib ditosylate (GW572016 ditosylate) is a potent 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) 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) 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) 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

4 °C, sealed storage, away from moisture and light *In solvent : -80 °C, 6 months; -20 °C, 1 month (sealed storage, away from moisture and light)

Shipping

Room temperature in continental US; may vary elsewhere.

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