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LapatinibEGFR/HER2 inhibitor,potent,selective and reversible

Lapatinib

Catalog No. A8218
Size Price Stock Qty
10mM (in 1mL DMSO) $55.00 In stock
Evaluation Sample $28.00 In stock
50mg $50.00 In stock
100mg $70.00 In stock

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Sample solution is provided at 25 µL, 10mM.

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Chemical structure

Lapatinib

Related Biological Data

Lapatinib

Related Biological Data

Lapatinib

Biological Activity

Description Lapatinib is a potent inhibitor of EGFR and ErbB2 with IC50 of 10.8 and 9.2 nM, respectively.
Targets EGFR ErbB2        
IC50 10.8 nM 9.2 nM        

Lapatinib Dilution Calculator

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Chemical Properties

Cas No. 231277-92-2 SDF Download SDF
Synonyms Tykerb;GW572016;GW-572016;GW 572016, Lapatinib tosilate hydrate
Chemical Name N-[3-chloro-4-[(3-fluorophenyl)methoxy]phenyl]-6-[5-[(2-methylsulfonylethylamino)methyl]furan-2-yl]quinazolin-4-amine
Canonical SMILES CS(=O)(=O)CCNCC1=CC=C(O1)C2=CC3=C(C=C2)N=CN=C3NC4=CC(=C(C=C4)OCC5=CC(=CC=C5)F)Cl
Formula C29H26ClFN4O4S M.Wt 581.06
Solubility Soluble in DMSO > 10 mM Storage Store at -20°C
General tips For obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while.Stock solution can be stored below -20℃ for several months.
Shipping Condition Evaluation sample solution : ship with blue ice
All other available size: ship with RT , or blue ice upon request

Background

Lapatinib (also known as GW572016), a member of the 4-anilinoquinazoline class of kinase inhibitors, is a potent, reversible and selective small-molecule inhibitor of both epidermal growth factor receptor (EGFR) and human epidermal growth factor receptor 2 (HER-2) tyrosine kinases that inhibits recombinant EGFR and HER-2 tyrosine kinases in cell-free biochemical kinase assays with values of 50% inhibition concentration IC50 of 10.8 nmol/L and 9.3 nmol/L respectively. Lapatinib interferes with the adenosine triphosphate binding in the tyrosine kinases domains of both EGFR and HER-2 resulting in the inhibition of auto-phosphorylation and resultant downstream signaling activities (such as cellular proliferation and survival).

Reference

Alison Reid, Laura Vidal, Heather Shaw and Johann de Bono. Dual inhibition of ErbB1 (EGFR/HER1) and ErbB2 (HER2/neu). European Journal of Cancer 43 (2007) 481-489

Norio Kondo, Mamoru Tsukuda, Yukari Ishiguro, Machiko Kimura, Kyoko Fujita, Atsuko Sakakibara, Hideaki Takahashi, Gabor Toth and Hideki Matsuda. Antitumor effects of lapatinib (GW572016), a dual inhibitor of EGFR and HER-2, in combination with cisplatin or paclitaxel on head and neck squamous cell carcinoma. Oncology Reports 23: 957-963, 2010

Zev A. Wainberg, Adrian Anghel, Amrita J. Desai, Raul Ayala, Tong Luo, Brent Safran, Marlena S. Fejzo, J. Randolph Hecht, Denni J. Slamon and Richard S. Finn. Lapatinib, a dual EGFR and HER2 kinase inhibitor, selectively inhibits HER2-amplified human gastric cancer cells and is synergistic with trastuzumab in vitro and in vivo. Clin Cancer Res 2010; 16(5): 1509-1519