General
Preferred name
LAPATINIB
Synonyms
Tykerb, Tyverb ()
Lapatinib ditosylate ()
GW-2016, GW-572016, GW572016F, Lapatinib Ditosylate, Tykerb, Lapatinib ditosylate monohydrate ()
GW-572016 ()
Tykerb ()
GSK572016 ()
GW572016 ()
Lapatinib ditoluenesulfonate monohydrate ()
Tyverb ditosylate monohydrate ()
Lapatinib ditosylate monohydrate ()
Lapatinib ditosilate hydrate ()
Tykerb ditosylate monohydrate ()
Lapatinib tosilate hydrate ()
Lapatinib (free base) ()
FMM ()
GSK 572016, Lapatinib ()
Lapatinib (ditosylate) ()
Lapatinib (ditosylate monohydrate) ()
GW2016 ()
GW572016 (ditosylate) ()
GW2016 (ditosylate) ()
GW572016 (ditosylate monohydrate) ()
GW2016 (ditosylate monohydrate) ()
GSK572016, GW2016 ()
Lapatinib ditoluenesulfonate monohydrate, Lapatinib tosilate, Lapatinib tosilate hydrate ()
Lapatinib (GW-572016) Ditosylate ()
Lapatinib (GW-572016) ()
Lapatinib free baseTykerbLapatinibGW 572016N-(3-Chloro-4-{[(3-fluorophenyl)methyl]oxy}phenyl)-6-[5-({[2-(methylsulfonyl)ethyl]amino}methyl)-2-furanyl]-4-quinazolinamine ()
GSK-572016 ()
GW-2016 ()
GW-572016X ()
Tyverb ()
Lapatinib ()
GW572016F ()
Lapatinib ditosylate anhydrous ()
Lapatinib tosilate ()
Tycerb ()
GW-572016F ()
Lapatanib ()
Lapatinib-d4 (tosylate) ()
P&D ID
PD003505
CAS
231277-92-2
388082-77-7
1092929-10-6
388082-78-8
2749856-05-9
Tags
available
probe
drug
Approved by
FDA
EMA
First approval
2007
Drug indication
Breast cancer
breast carcinoma
Neoplasm
Drug Status
approved
investigational
Max Phase
4.0
Probe info
Probe type
P&D approved
experimental probe
Probe selectivity
family-selective
Probe sources
Probe targets
[[ compound.targets[t].gene_name ]]
Probe control
Probe control not defined
Orthogonal probes
110
No orthogonal probes found
Similar probes
16
No structurally similar probes found
Structure
P&D probe-likeness score
Structure formats
[[ format ]]
[[ compound[format === 'MOL' ? 'molblock' : format.toLowerCase()] ]]
Description
(extracted from source data)
HALF-LIFE
Single-dose terminal half life: 14.2 hours; Effective multiple-dose half life: 24 hours
DESCRIPTION
Lapatinib is a Type-1.5 kinase inhibitor and was first approved by the US FDA in 2007.
(GtoPdb)
DESCRIPTION
Lapatinib (GW572016) is a potent inhibitor of the ErbB-2 and EGFR tyrosine kinase domains with IC50 values against purified EGFR and ErbB-2 of 10.2 and 9.8 nM, respectively[1].
PRICE
29
DESCRIPTION
Lapatinib ditosylate (GW572016 ditosylate) is a potent inhibitor of the ErbB-2 and EGFR tyrosine kinase domains with IC50 values against purified EGFR and ErbB-2 of 10.2 and 9.8 nM, respectively[1].
DESCRIPTION
Lapatinib ditosylate monohydrate (GW572016 ditosylate monohydrate) is a potent inhibitor of the ErbB-2 and EGFR tyrosine kinase domains with IC50 values against purified EGFR and ErbB-2 of 10.2 and 9.8 nM, respectively[1].
MOA
Inhibitor
(Chemical Probes.org)
DESCRIPTION
inhibitor of EGFR and HER2
(Informer Set)
DESCRIPTION
Indicated in combination with capecitabine for the treatment of patients with advanced or metastatic breast cancer whose tumors overexpress the human epidermal receptor type 2 (HER2) protein and who have received prior therapy including an anthracycline, a taxane, and trastuzuma.
(PKIDB)
DESCRIPTION
Potent dual specificity EGFR/HER2 inhibitor; active in vivo
(Tocris Bioactive Compound Library)
DESCRIPTION
Lapatinib is a 4-anilinoquinazoline kinase inhibitor of the intracellular tyrosine kinase domains of both epidermal growth factor receptor (HER1/EGFR/ERBB1) and human epidermal growth factor receptor type 2 (HER2/ERBB2). Lapatinib is an anti-cancer drug, used for the treatment for solid tumours such as breast and lung cancer.
(Enamine Bioactive Compounds)
DESCRIPTION
Lapatinib (GW572016) is an inhibitor of ErbB2 and EGFR (IC50=9.2/10.8 nM) with oral activity. Lapatinib has antitumor activity and can be used to treat advanced or metastatic breast cancer with HER2 overexpression.
(TargetMol Bioactive Compound Library)
DESCRIPTION
Lapatinib ditosylate (Lapatinib tosilate) monohydrate is a tyrosine kinase receptor inhibitor used in the therapy of advanced breast cancer and other solid tumors. Lapatinib ditosylate monohydrate therapy is associated with transient elevations in serum aminotransferase levels and rare instances of clinically apparent acute liver injury.
(TargetMol Bioactive Compound Library)
[[ p.pathway_name ]]
[[ compound.targets[tid].gene_name ]]
Cell lines
217
Organisms
4
Compound Sets
40
Axon Medchem Screening Library
ChEMBL Approved Drugs
ChEMBL Drugs
Chemical Probes.org
Clinical kinase drugs
Concise Guide to Pharmacology 2017/18
CZ-OPENSCREEN Bioactive Library
Drug Repurposing Hub
DrugBank
DrugBank Approved Drugs
DrugCentral
DrugCentral Approved Drugs
DrugMAP
DrugMAP Approved Drugs
Enamine Bioactive Compounds
Enamine BioReference Compounds
EU-OPENSCREEN Bioactive Compound Library
EUbOPEN Chemogenomics Library
Guide to Pharmacology
High-quality chemical probes
Informer Set
LSP-MoA library (Laboratory of Systems Pharmacology)
LSP-OptimalKinase library (Laboratory of Systems Pharmacology)
NCATS Inxight Approved Drugs
NIH Approved Oncology Drugs
Novartis Chemogenetic Library (NIBR MoA Box)
NPC Screening Collection
Other bioactive compounds
PKIDB
ReFrame library
Selleckchem Bioactive Compound Library
The Spectrum Collection
Tocris Bioactive Compound Library
VGSC-DB
Welcome Trust Cancer Drugs
[[ a.name ]]
[[ ligand_id ]]
free of charge
External IDs
83
Molecular Weight
580.13
Hydrogen Bond Acceptors
8
Hydrogen Bond Donors
2
Rotatable Bonds
11
Ring Count
5
Aromatic Ring Count
5
cLogP
6.14
TPSA
106.35
Fraction CSP3
0.17
Chiral centers
0.0
Largest ring
6.0
QED
0.18
Structural alerts
0
No structural alerts detected
Related compounds
Custom attributes
(extracted from source data)
Target
EGFR
ERBB2
EGFR, ERBB2
EGFR/ErbB-2 inhibitor
Ferroptosis
EGFR,HER2
Autophagy,EGFR,Ferroptosis,HER2
HER2
HER2/ErbB2
Compound status
FDA
Pathway
EGFR signaling
Angiogenesis
Apoptosis
Autophagy
JAK/STAT Signaling
Tyrosine Kinase/Adaptors
Protein Tyrosine Kinase/RTK
Targets
EGFR,ERBB2
MOA
EGFR inhibitor
Inhibitor
EGFR (HER1
erbB1) Inhibitors
HER2 (erbB2) Inhibitors
Inhibitors of Signal Transduction Pathways
Member status
member
Indication
breast cancer
Target subclass
RTK
RTK, RTK
Target class
Protein kinase
Kinase, Kinase
Orthogonal probe
Canertinib
Therapeutic Class
Anticancer Agents
VGSC Target
Nav1.5
Recommended Cell Concentration
1 uM
Source data
