General
Preferred name
Tucatinib
Synonyms
ONT-380, Irbinitinib, Tucatinib ()
ARRY-380 ()
Irbinitinib ()
ONT-380 ()
ONT-380 hemiethanolate ()
ARRY-380 hemiethanolate ()
Irbinitinib hemiethanolate ()
Tucatinib (hemiethanolate) ()
Irbinitinib (hemiethanolate) ()
ARRY-380 (hemiethanolate) ()
ONT-380 (hemiethanolate) ()
Irbinitinib, ONT-380, ARRY-380 ()
Tucatinib hemiethanolate ()
WA024-00ARRY-380N6-(4,4-Dimethyl-4,5-dihydro-oxazol-2-yl)-N4[3-methyl-4-([1,2,4]triazolo[1,5-a]pyridin-7-yloxy)-phenyl]-quinazoline-4,6-diamine ()
MK-7119 ()
TUKYSA ()
P&D ID
PD056028
CAS
937263-43-9
1429755-56-5
Tags
available
drug
Approved by
FDA
EMA
First approval
2020
Drug indication
Liver disease
Gastric adenocarcinoma
HER2-positive breast cancer
Drug Status
approved
investigational
Max Phase
4.0
Probe control
Probe control not defined
Orthogonal probes
0
No orthogonal probes found
Similar probes
0
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)
DESCRIPTION
Tucatinib is an orally bioavailable ERBB2 (HER2) receptor tyrosine kinase inhibitor that was developed as a novel antineoplastic agent by Seattle Genetics . The chemical structure is claimed as Example 11 in Array Biopharma patent WO2007059257A2 , and was exemplified as ARRY-380 in the later patent WO2013056183A1 . Tucatinib contains a quinazoline core that is conserved in other tyrosine kinase inhibitors including , , and .
The INN tucatinib replaced the earlier INN irbinitinib that was associated with this chemical entity. (GtoPdb)
The INN tucatinib replaced the earlier INN irbinitinib that was associated with this chemical entity. (GtoPdb)
DESCRIPTION
Tucatinib (Irbinitinib) is a potent, orally active and selective HER2 inhibitor with an IC50 of 8 nM.
PRICE
69
DESCRIPTION
Tucatinib (Irbinitinib) hemiethanolate is a potent, orally active and selective HER2 inhibitor with an IC50 of 8 nM.
DESCRIPTION
On April 2020, FDA approved tucatinib to treat advanced unresectable or metastatic HER2-positive breast cancer.
(PKIDB)
DESCRIPTION
Tucatinib (ONT-380) is a potent and selective HER2 inhibitor (IC50: 8 nM).
(TargetMol Bioactive Compound Library)
DESCRIPTION
Tucatinib (Irbinitinib) hemiethanolate is a potent, orally active, and selective HER2 inhibitor with an IC50 of 8 nM.
(TargetMol Bioactive Compound Library)
[[ p.pathway_name ]]
[[ compound.targets[tid].gene_name ]]
Compound Sets
20
AdooQ Bioactive Compound Library
Cayman Chemical Bioactives
ChEMBL Approved Drugs
ChEMBL Drugs
Clinical kinase drugs
Drug Repurposing Hub
DrugBank
DrugBank Approved Drugs
DrugCentral
DrugCentral Approved Drugs
DrugMAP
DrugMAP Approved Drugs
Guide to Pharmacology
NCATS Inxight Approved Drugs
NIH Approved Oncology Drugs
PKIDB
ReFrame library
Selleckchem Bioactive Compound Library
[[ a.name ]]
[[ ligand_id ]]
free of charge
External IDs
29
Molecular Weight
480.2
Hydrogen Bond Acceptors
10
Hydrogen Bond Donors
2
Rotatable Bonds
5
Ring Count
6
Aromatic Ring Count
5
cLogP
5.09
TPSA
110.85
Fraction CSP3
0.19
Chiral centers
0.0
Largest ring
6.0
QED
0.36
Structural alerts
0
No structural alerts detected
Related compounds
Custom attributes
(extracted from source data)
Targets
ERBB2
Target
EGFR
HER2/ErbB2
p95 HER2
HER2
EGFR,HER2
MOA
EGFR inhibitor
Pathway
Angiogenesis
JAK/STAT Signaling
Tyrosine Kinase/Adaptors
Protein Tyrosine Kinase/RTK
Source data
