Lapatinib

Catalog No.S2111

Lapatinib, used in the form of Lapatinib Ditosylate, is a potent EGFR and ErbB2 inhibitor with IC50 of 10.8 and 9.2 nM in cell-free assays, respectively.

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Lapatinib Chemical Structure

Lapatinib Chemical Structure
Molecular Weight: 581.06

Validation & Quality Control

Product Use Citation(35)

Customer Product Validation(7)

Quality Control & MSDS

Related Compound Libraries

Lapatinib is available in the following compound libraries:

EGFR Inhibitors with Unique Features

  • Selective EGFR Inhibitor

    Erlotinib HCl (OSI-744) EGFR-selective, IC50=2 nM.

  • Most Potent EGFR Inhibitor

    Afatinib (BIBW2992) EGFR(wt), IC50=0.5 nM; EGFR(L858R), IC50=0.4 nM; EGFR(L858R/T790M), IC50=10 nM; HER2, IC50=14 nM.

  • FDA-approved EGFR Inhibitor

    Gefitinib (ZD1839) Approved by FDA for NSCLC.

  • Newest EGFR Inhibitor

    CO-1686 (AVL-301) Irreversible, mutant-selective EGFR inhibitor with Ki of 21.5 nM and 303.3 nM for EGFRL858R/T790M and EGFRWT, respectively.

Product Information

  • Compare EGFR Inhibitors
    Compare EGFR Products
  • Research Area

Product Description

Biological Activity

Description Lapatinib, used in the form of Lapatinib Ditosylate, is a potent EGFR and ErbB2 inhibitor with IC50 of 10.8 and 9.2 nM in cell-free assays, respectively.
Targets ErbB2 [1]
(Cell-free assay)
EGFR [1]
(Cell-free assay)
ErbB4 [1]
(Cell-free assay)
c-Src [1]
(Cell-free assay)

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IC50 9.2 nM 10.8 nM 367 nM 3.5 μM
In vitro Lapatinib weakly inhibits the activity of ErbB4 with IC50 of 367 nM, and displays >300-fold selectivity for EGFR and ErbB2 over other kinases such as c-Src, c-Raf, MEK, ERK, c-Fms, CDK1, CDK2, p38, Tie-2, and VEGFR2. Lapatinib significantly inhibits receptor autophosphorylation of EGFR and ErbB2 in a dose-dependent manner with IC50 of 170 nM and 80 nM, respectively in HN5 cells; as well as 210 nM and 60 nM, respectively in BT474 cells. Unlike OSI-774 and Iressa (ZD1839) which preferentially inhibit the growth of the EGFR-overexpressing cells, Lapatinib inhibits the growth of both EGFR- and ErbB2-overexpressing cells. Lapatinib displays higher inhibitory activity against EGFR- or ErbB2-overexpressing cells with IC50 of 0.09-0.21 μM, compared with cells expressing low levels of EGFR or ErbB2 with IC50 of 3-12 μM, and exhibits ~100-fold selectivity over the normal fibroblast cells. Lapatinib potently inhibits the outgrowth of EGFR-overexpressing HN5 and A-431 cells, as well as ErbB2-overexpressing BT474 and N87 cells, and significantly induces G1 arrest of HN5 cells and apoptosis of BT474 cells, which are associated with inhibition of AKT phosphorylation. [1]
Cell Data
Cell LinesAssay TypeConcentrationIncubation TimeFormulationActivity DescriptionPMID
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EB2M{X4fGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7NFrFZopKSzVyPUO2MlYyQDlizszNNHnxZYJUSU6JRWK=
L-540MonPS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl?M3fzRmlEPTB;M{euNlMxQCEQvF2=MWDTRW5ITVJ?
NCI-H747NWL0PGN4T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm=NUL5b203UUN3ME2zPE45QDR4IN88US=>NIPVcnNUSU6JRWK=
NCI-H446MWPHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>?NYTNe5BbUUN3ME2zPU46PjVzIN88US=>MkH5V2FPT0WU
MOLT-16NXzQcXlUT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm=MkK2TWM2OD12Mj60NVUh|ryPMYfTRW5ITVJ?
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SJSA-1MXjHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>?NGPIVJlKSzVyPUS1MlU1PzRizszNNVPXR5o2W0GQR1XS
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SNB75M1nnUWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7MoPsTWM2OD12Nj6wNVgh|ryPNVPVOVdTW0GQR1XS

... Click to View More Cell Line Experimental Data

In vivo Oral administration of Lapatinib (~100 mg/kg) twice daily significantly inhibits the growth of BT474 and HN5 xenografts in a dose-dependent manner. [1]
Features

Protocol(Only for Reference)

Kinase Assay: [1]

In vitro kinase assays The IC50 values for inhibition of enzyme activity are generated by measuring inhibition of phosphorylation of a peptide substrate. The intracellular kinase domains of EGFR and ErbB2 are purified from a baculovirus expression system. EGFR and ErbB2 reactions are performed in 96-well polystyrene round-bottomed plates in a final volume of 45 μL. Reaction mixtures contain 50 mM 4-morpholinepropanesulfonic acid (pH 7.5), 2 mM MnCl2, 10 μM ATP, 1 μCi of [γ33P] ATP/reaction, 50 μM Peptide A [Biotin-(amino hexonoic acid)-EEEEYFELVAKKK-CONH2], 1 mM dithiothreitol, and 1 μL of DMSO containing serial dilutions of Lapatinib beginning at 10 μM. The reaction is initiated by adding the indicated purified type-1 receptor intracellular domain. The amount of enzyme added is 1 pmol/reaction (20 nM). Reactions are terminated after 10 minutes at 23°C by adding 45 μL of 0.5% phosphoric acid in water. The terminated reaction mix (75 μL) is transferred to phosphocellulose filter plates. The plates are filtered and washed three times with 200 μL of 0.5% phosphoric acid. Scintillation cocktail (50 μL) is added to each well, and the assay is quantified by counting in a Packard Topcount. IC50 values are generated from 10-point dose-response curves.

Cell Assay: [1]

Cell lines HFF, MCF-7, T47D, A-431, HN5, BT474, N87, CaLu-3, HB4a, and HB4a c5.2 cells
Concentrations Dissolved in DMSO, final concentrations ~100 μM
Incubation Time 72 hours
Method Cells are exposed to various concentrations of Lapatinib for 72 hours. Relative cell number is estimated using methylene blue staining. The absorbance at 620 nm is read in a Spectra microplate reader. Cell death and cell cycle analysis are assessed by propidium iodide staining and antibody detection of incorporated BrdUrd and staining with propidium iodide.

Animal Study: [1]

Animal Models CD-1 nude female mice implanted s.c. with HN5 cells, and C.B-17 SCID female mice implanted s.c. with BT474 cells
Formulation Formulated in a vehicle of sulfo-butyl-ether-β-cyclodextrin 10% aqueous solution (CD10)
Dosages ~100 mg/kg
Administration Orally twice daily

Conversion of different model animals based on BSA (Value based on data from FDA Draft Guidelines)

SpeciesMouseRatRabbitGuinea pigHamsterDog
Weight (kg)0.020.151.80.40.0810
Body Surface Area (m2)0.0070.0250.150.050.020.5
Km factor36128520
Animal A (mg/kg) = Animal B (mg/kg) multiplied by  Animal B Km
Animal A Km

For example, to modify the dose of resveratrol used for a mouse (22.4 mg/kg) to a dose based on the BSA for a rat, multiply 22.4 mg/kg by the Km factor for a mouse and then divide by the Km factor for a rat. This calculation results in a rat equivalent dose for resveratrol of 11.2 mg/kg.

Rat dose (mg/kg) = mouse dose (22.4 mg/kg) ×  mouse Km(3)  = 11.2 mg/kg
rat Km(6)
1

References

[1] Rusnak DW, et al. Mol Cancer Ther, 2001, 1(2), 85-94.

Clinical Trial Information( data from http://clinicaltrials.gov, updated on 2016-05-29)

NCT Number Recruitment Conditions Sponsor
/Collaborators
Start Date Phases
NCT02650752 Recruiting Metastatic Breast Cancer|Central Nervous System (CNS) Metastases Memorial Sloan Kettering Cancer Center|Queens Cancer Cent  ...more Memorial Sloan Kettering Cancer Center|Queens Cancer Center of Queens Hospital|University of Michigan January 2016 Phase 1
NCT02581124 Completed Anemia of Chronic Kidney Disease Akros Pharma Inc. October 2015 Phase 1
NCT02559778 Recruiting Neuroblastoma Giselle Sholler|Dell, Inc.|Beat NB Cancer Foundation|Beca  ...more Giselle Sholler|Dell, Inc.|Beat NB Cancer Foundation|Because of Ezra|Spectrum Health Hospitals September 2015 Phase 1
NCT02422199 Not yet recruiting HER2 Positive Metastatic Breast Cancer Jiangsu HengRui Medicine Co., Ltd. May 2015 Phase 1|Phase 2
NCT02362958 Recruiting HER2 Positive Breast Cancer Sun Yat-sen University February 2015 Phase 2

view more

Chemical Information

Download Lapatinib SDF
Molecular Weight (MW) 581.06
Formula

C29H26ClFN4O4S

CAS No. 231277-92-2
Storage 3 years -20℃powder
6 months-80℃in solvent
Synonyms GW-572016, GSK572016
Solubility (25°C) * In vitro DMSO 100 mg/mL (172.09 mM)
Water <1 mg/mL (<1 mM)
Ethanol <1 mg/mL (<1 mM)
In vivo 2% DMSO+30% PEG 300+5% Tween 80+ddH2O 10mg/mL
* <1 mg/ml means slightly soluble or insoluble.
* Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations.
Chemical Name N-(4-(3-fluorobenzyloxy)-3-chlorophenyl)-6-(5-((2-(methylsulfonyl)ethylamino)methyl)furan-2-yl)quinazolin-4-amine,di4-methylbenzenesulfonate

Customer Product Validation (7)


Click to enlarge
Rating
Source Cancer Cell 2012 21(4), 488-503. Lapatinib purchased from Selleck
Method Cell Proliferation Assay
Cell Lines Primary Cancer Cells from Different Tumor Stages
Concentrations 1, 10 uM
Incubation Time 48 h
Results In vitro sensitivity to theErbB1/ErbB2 inhibitor lapatinib was highest for cells isolatedfrom late carcinomas.

Click to enlarge
Rating
Source Cancer Lett 2013 340(1), 43-50. Lapatinib purchased from Selleck
Method Western blot
Cell Lines SK-BR-3-LR cells
Concentrations 0.1 uM
Incubation Time 24 h
Results Aberrantly activated PI3K/AKT pathway mediates lapatinib resistance in SK-BR-3-LR cells.

Click to enlarge
Rating
Source Mol Oncol 2013 7(3), 392-401. Lapatinib purchased from Selleck
Method siRNAs
Cell Lines KPL4 cells
Concentrations 100 nM
Incubation Time 72 h
Results Wecompared the efficacy of siHER2 to trastuzumab and Lapatinibtreatment and the combination of these and observed a similarresponse pattern between the siHER2 and the drug treatmentswith trastuzumab alone being least efficient

Click to enlarge
Rating
Source Mol Carcinog 2013 52(12), 959-69. Lapatinib purchased from Selleck
Method Western blot
Cell Lines MDA-MB-468 cells
Concentrations 25 uM
Incubation Time 24 h
Results Lapatinib effectively inhibits EGFR activation, leading to a reduction in STAT1 expression.

Click to enlarge
Rating
Source Mol Carcinog 2012 52, 959-69. Lapatinib purchased from Selleck
Method Western Blot
Cell Lines MDA-MB-468 cells
Concentrations 25 uM
Incubation Time 24 h
Results lapatinib effectively inhibits EGFR activation, leading to a reduction in STAT1 expression.

Click to enlarge
Rating
Source Acta Pharmacol Sin 2013 10.1038/aps.2013.124. Lapatinib purchased from Selleck
Method Western blot
Cell Lines H195 cells
Concentrations 1 uM
Incubation Time 24 h
Results Combination treatmentwith lapatinib and CZ0775significantly induces pro-apoptotic BIM proteins in H195cells.

Click to enlarge
Rating
Source Anticancer Res 2011 31, 3767-3774. Lapatinib purchased from Selleck
Method Real time PCR/Western Blot
Cell Lines SKBR3 cells
Concentrations 2 μM
Incubation Time 30 min
Results Both EGF and TGF-α significantly increased the level of CD44 mRNA expression . However, EGF- or TGF-α-induced CD44 mRNA expression was reduced by EGFR inhibitors …. EGF-induced CD44 protein expression was reduced by both AG1478 and lapatinib.

Tech Support

Answers to questions you may have can be found in the inhibitor handling instructions. Topics include how to prepare stock solutions, how to store inhibitors, and issues that need special attention for cell-based assays and animal experiments.

Tel: +1-832-582-8158 Ext:3

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