General
Preferred name
Lazertinib
Synonyms
Lazertinib (YH25448) ()
GNS-1480 ()
YH25448 ()
Lazertinib (mesylate) ()
YH25448 (mesylate) ()
GNS-1480 (mesylate) ()
YH25448,GNS-1480 ()
LAZERTINIB MESYLATE ()
C-18112003-G ()
GNS1480 ()
JNJ-73841937-AAA ()
YH-25448 ()
Lazertinib mesylate monohydrate ()
YH25448AM ()
R-605024 ()
JNJ-73841937-ZCY ()
Lazcluze ()
Leclaza ()
R605024 ()
Lazertinib mesilate hydrate ()
P&D ID
PD087750
CAS
2247995-37-3
1903008-80-9
Tags
available
drug
Drug Status
approved
investigational
Max Phase
4.0
Drug indication
Neoplasm
non-small cell lung carcinoma
First approval
2024
Structure
Probe scores
P&D probe-likeness score
[[ v.score ]]%
Structure formats
[[ format ]]
[[ compound[format === 'MOL' ? 'molblock' : format.toLowerCase()] ]]
Description
(extracted from source data)
DESCRIPTION Lazertinib (YH-25448, GNS-1480) is an oral, third-generation inhibitor of the aberrant activity of mutant EGFR kinases (EGFR T790M and the activating EGFR mutations Ex19del and L858R), that was originally developed by Yuhan Corporation for antineoplastic potential in cancers with (acquired) resistance to existing EGFR tyrosine kinase inhibitors , in particular for EGFR mutation positive, advanced non-small cell lung cancer (NSCLC). It is claimed in Yuhan's patent WO2016060443A2 as compound 73 .
In addition to predicted efficacy for the treatment of primary lung and extracranial lesions, lazertinib is expected to be beneficial for NSCLC brain metastases as it is able to cross the blood brain barrier. (GtoPdb)
PRICE 160
DESCRIPTION Lazertinib (YH-25448, GNS-1480) is an inhibitor of the aberrant activity of EGFR mutant kinases, that was originally developed by Yuhan Corporation for antineoplastic potential in cancers with (acquired) resistance to existing EGFR tyrosine kinase inhibitors, in particular for EGFR mutation positive, advanced non-small cell lung cancer (NSCLC). In addition to predicted efficacy for the treatment of primary lung and extracranial lesions, lazertinib is expected to be beneficial for NSCLC brain metastases as it is able to cross the blood brain barrier. (PKIDB)
DESCRIPTION Lazertinib (GNS-1480) is an effective, highly mutant-selective and irreversible EGFR-TKI with IC50 values of 1.7 nM, 2 nM, 5 nM, 20.6 nM and 76 nM for Del19/T790M, L858R/T790M, Del19, L85R and Wild type EGFR respectively. (TargetMol Bioactive Compound Library)
Cell lines
3
Organisms
0
Compound Sets
13
Cayman Chemical Bioactives
29670
ChEMBL Approved Drugs
CHEMBL4558324
CHEMBL6068478
ChEMBL Drugs
CHEMBL4558324
CHEMBL6068478
Drug Repurposing Hub
DrugBank
DB16216
DrugBank Approved Drugs
DB16216
EU-OPENSCREEN Bioactive Compound Library
EOS100261
EUbOPEN Chemogenomics Library
EUB0002108
Guide to Pharmacology
10136
MedChem Express Bioactive Compound Library
HY-109061
HY-109061B
PKIDB
Selleckchem Bioactive Compound Library
lazertinib-yh25448-gns-1480
TargetMol Bioactive Compound Library
T4485
External IDs
20
Properties
(calculated by RDKit )
Molecular Weight
554.28
Hydrogen Bond Acceptors
10
Hydrogen Bond Donors
2
Rotatable Bonds
10
Ring Count
5
Aromatic Ring Count
4
cLogP
4.1
TPSA
109.67
Fraction CSP3
0.27
Chiral centers
0.0
Largest ring
6.0
QED
0.28
Structural alerts
0
No structural alerts detected
Related compounds
Custom attributes
(extracted from source data)
Target
EGFR
EGFR (del19)
EGFR (T790M)
EGFR (T790M/L858R)
EGFR (wildtype)
Akt
ERK
MOA
EGFR inhibitor
tyrosine kinase inhibitor
Pathway
JAK/STAT Signaling
MAPK/ERK Pathway
PI3K/Akt/mTOR
Protein Tyrosine Kinase/RTK
Stem Cell/Wnt
Angiogenesis
Tyrosine Kinase/Adaptors
Recommended Cell Concentration
1 uM
Source data