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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.

Product Citations

1. Zhang WJ, Li Y, et al. "Synergistic antitumor activity of regorafenib and lapatinib in preclinical models of human colorectal cancer." Cancer Lett. 2017 Feb 1;386:100-109. PMID:27864115

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Chemical structure

Lapatinib

Related Biological Data

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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Lapatinib Molarity 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 >29.1mg/mL in DMSO 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