Lapatinib

Protein target name:

EGFR, ERBB2

Mechanism of action:

Inhibitor

Recommended Concentration for use in cells:

up to 10 uM

Probe Availability

Probe Information

Target and Probe Information

Target Details

Target class:

Protein kinase

Subclass:

RTK

HUGO ID:

HGNC:3236 HGNC:3430

Entrez gene ID:

1956 2064

UNIPROT ID:

P00533 P04626

Target alias:

ERBB; HER1; mENA; ERBB1; PIG61; NISBD2; NEU; NGL; HER2; TKR1; CD340; HER-2; MLN 19; HER-2/neu

Probe Details

Chemical Probes Portal ID:

CPP2193

Probe alias:

GSK-572016, GW572016, GW-2016, Tyverb, FMM

PubChem CID:

208908

ChEMBL ID:

CHEMBL554

SMILES string:

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

InChi Key:

BCFGMOOMADDAQU-UHFFFAOYSA-N

Orthogonal probe:

CanertinibAfatinibSJF1528

Validation in Cells and Model Organisms

In vitro validation

On target activity

Potency:

IC50

10.2 nM EGFR9.8 nM ERBB2

Potency assay:

In vitro kinase assay using intracellular kinase domain

PDB ID for probe-target interaction (3D structure):

1XKK

Structure-activity relationship:

yes

Off target activity

Potency (off target):

IC50

Off target protein and potency:

367 nM ERBB4

Potency assay (off target):

In vitro kinase activity

Probe Selectivity in Vitro:

enzyme inhibitory activity reveal, C-Src IC50 3500 and IC50 > 10000 nM for c-Raf-1, MEK. ERK, c-Fms, CDK1, CDK2, p38, Tie-2, VEGFR-2

In cell validation

On target activity in cells

Potency in cells:

IC50

170 nM EGFR80 nM ERBB2

Potency assay (cells):

Autophosphorylation Inhibition (immunoprecipitation and WB), Cell growth inhibition

In vivo validation

Organism:

CD-1 nude female miceC.B-17 SCID female mice

Dose:

30-100 mg/Kg

Route of delivery:

Oral

Primary Reference

Reference (PMID):

12467226

Lapatinib

Probe Availability

Probe Information

Target Details

ERBB; HER1; mENA; ERBB1; PIG61; NISBD2; NEU; NGL; HER2; TKR1; CD340; HER-2; MLN 19; HER-2/neu

Probe Details

In vitro validation

In cell validation

In vivo validation

Primary Reference

Supporting Organizations

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Lapatinib

Probe Availability

Probe Information

Target Details

ERBB; HER1; mENA; ERBB1; PIG61; NISBD2; NEU; NGL; HER2; TKR1; CD340; HER-2; MLN 19; HER-2/neu

Probe Details

In vitro validation

In cell validation

In vivo validation

Primary Reference

Supporting Organizations

Interested in supporting the portal?