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Lapatinib Ditosylate Monohydrate
Cat. No. IC23172
CAS. No. 388082-78-8
Key Features and Details
Category
Inhibitor&Activator
Purity
99.78%
Formula
C43H44ClFN4O11S3
Product Details
Product Name
Lapatinib Ditosylate Monohydrate
CAS No.
388082-78-8
Molecular Weight
943.48
Synonyms
GW572016 ditosylate monohydrate; GW2016 ditosylate monohydrate
Formula
C43H44ClFN4O11S3
Appearance
Solid
Purity
99.78%
SMILES
O=S(CCNCC1=CC=C(C2=CC3=C(NC4=CC=C(OCC5=CC=CC(F)=C5)C(Cl)=C4)N=CN=C3C=C2)O1)(C)=O.O=S(C6=CC=C(C)C=C6)(O)=O.O=S(C7=CC=C(C)C=C7)(O)=O.O
Product Overview
Description
Lapatinib ditosylate monohydrate (GW572016 ditosylate monohydrate) 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
In solvent : -80 °C, 6 months; -20 °C, 1 month (sealed storage, away from moisture)
Shipping
Room temperature in continental US; may vary elsewhere.
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