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Lapatinib DitosylateEGFR/HER2 inhibitor,potent and selective

Lapatinib Ditosylate

Catalog No. A3967
Size Price Stock Qty
10mM (in 1mL DMSO) $105.00 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 Ditosylate

Related Biological Data

Lapatinib Ditosylate

Related Biological Data

Lapatinib Ditosylate

Biological Activity

Description Lapatinib Ditosylate (GW572016, GW2016) 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        

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Chemical Properties

Cas No. 388082-78-8 SDF Download SDF
Synonyms Tykerb Ditosylate
Chemical Name N-[3-chloro-4-[(3-fluorophenyl)methoxy]phenyl]-6-[5-[(2-methylsulfonylethylamino)methyl]furan-2-yl]quinazolin-4-amine;4-methylbenzenesulfonic acid;hydrate
Canonical SMILES CC1=CC=C(C=C1)S(=O)(=O)O.CC1=CC=C(C=C1)S(=O)(=O)O.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 2C7H8O3S M.Wt 925.46
Solubility >24.3mg/mL in DMSO Storage Store at RT
General tips N/A
Shipping Condition N/A

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Research Update

1. Lapatinib ditosylate: expanding therapeutic options for receptor tyrosine-protein kinase erbB-2-positive breast cancer. Drugs Today (Barc). 2011 May;47(5):335-45. doi: 10.1358/dot.2011.47.5.1584110.
Abstract
Lapatinib ditosylate is a tyrosine kinase inhibitor targeting HER2 receptor that exhibits activity in transtuzumab-resistant advanced tumors, recurrent local advanced inflammatory breast cancer and brain metastases. The combination of lapatinib ditosylate , trastuzumab and paclitaxel significantly improved pathological complete response in Neo-ALTTO trails.
2. RON confers lapatinib resistance in HER2-positive breast cancer cells. Cancer Lett. 2013 Oct 28;340(1):43-50. doi: 10.1016/j.canlet.2013.06.022. Epub 2013 Jun 27.
Abstract
RON plays an important role in lapatinib-resistance mediation, where small-molecular RON inhibitors and siRNA could restore lapatinib sensitivity in SK-BR-3-LR cells.
4. Lapatinib as a component of neoadjuvant therapy for HER2-positive operable breast cancer (NSABP protocol B-41): an open-label, randomised phase 3 trial. Lancet Oncol. 2013 Nov;14(12):1183-92. doi: 10.1016/S1470-2045(13)70411-X. Epub 2013 Oct 4.
Abstract
Lapatinib plus paclitaxel and lapatinib plus trastuzumab were evaluated respectively for their effects on tumor response in HER2+ breast cancer patients with prior treatment of doxorubicin plus cyclophosphamide.
5. Addition of amino acid moieties to lapatinib increases the anti-cancer effect via amino acid transporters. Biopharm Drug Dispos. 2014 Jan;35(1):60-9. doi: 10.1002/bdd.1872. Epub 2013 Nov 19.
Abstract
The enhanced anticancer activity of val-lapatinib and tyr-lapatinib in various cancer cells, including human breast cancer cells and lung cancer cells, is possible caused by increased uptake of them into cancer cells via amino acid transporter, since they were found to inhibited glutamine transport in cancer cells.

Background

Lapatinib Ditosylateis a selective dual inhibitor of ErbB-2 and EGFR with IC50 value against ErbB-2 and EGFR of 9.8 and 10.2 nM in vitro, respectively. [1]
The EGFR and ErbB-2 all are the type I receptor tyrosine kinase that exists on the cell surface and have been recognised as potential targets for cancers. A conformational change happens by binding of its specific ligands in the receptor then activates the kinase domain. Whereas, erbB2 is generally thought that it has no known direct activating ligand, and it may become active by heterodimerization with other ligand-bound family members. EGFR dimerization stimulates protein-tyrosine kinase activity and elicits downstream signaling by several other proteins. These proteins initiate several signal transduction pathway. EGFR and ErbB-2 are well known to stimulate cell division through the Ras pathway, and resulting in cell growth through the PI3K pathway. [1]
Lapatinib is a selective inhibitor of the ErbB-2 and EGFR. Lapatinib was>300 fold selective for ErbB-2 and EGFR over other kinases, such as MEK, ERK. Lapatinib likely competed intracellular ATP with Erb-2 and EGFR,then inhibit the activation of them. Lapatinib inhibited the growth of human tumor cells in a cell-based proliferation assay. The IC50 values was < 0.16nM in the ErbB-2- and EGFR -overexpressing cell lines: HN5, A-431. In the cell lines expressing low level ErbB-2- and EGFR. The IC50 values were about 25-fold higher than in the overexpressing cell lines. Lapatinib resulted in G1 arrest at 10nM in HN5 cells. Lapatinib inhibited phos phorylated Er k1/2 100% at 5 nM in an erbB2 overexpressing cell line. Lapatinib inhibited EGF stimulated p-Erk1/ 2 at 1 nM and complet ely inh ibited p-AKT.[1, 2]
In human breast cancer xenografts, tumor volumes in mice at the dose of 75 mg/kg of lapatinib twice daily were significantly smaller than the vehicle control, at day 21.[3] Lapatinib completely inhibited the growth of HN5 and BT474 human tumor xenografts at the 100 mg/kg dose, twice daily.[1]
References:
1.Rusnak DW, Lackey K, Affleck K, Wood ER, Alligood KJ, Rhodes N, Keith BR, Murray DM, Knight WB, Mullin RJ et al: The effects of the novel, reversible epidermal growth factor receptor/ErbB-2 tyrosine kinase inhibitor, GW2016, on the growth of human normal and tumor-derived cell lines in vitro and in vivo. Mol Cancer Ther 2001, 1(2):85-94.
2.Xia W, Mullin RJ, Keith BR, Liu LH, Ma H, Rusnak DW, Owens G, Alligood KJ, Spector NL: Anti-tumor activity of GW572016: a dual tyrosine kinase inhibitor blocks EGF activation of EGFR/erbB2 and downstream Erk1/2 and AKT pathways. Oncogene 2002, 21(41):6255-6263.
3.Konecny GE, Pegram MD, Venkatesan N, Finn R, Yang G, Rahmeh M, Untch M, Rusnak DW, Spehar G, Mullin RJ et al: Activity of the dual kinase inhibitor lapatinib (GW572016) against HER-2-overexpressing and trastuzumab-treated breast cancer cells. Cancer Res 2006, 66(3):1630-1639.