General
Preferred name
Selpercatinib
Synonyms
LOXO-292 ()
WHO 10967 ()
Selpercatinib (LOXO-292) ()
6-(2-hydroxy-2-methylpropoxy)-4-(6-{6-[(6-methoxypyridin-3-yl)methyl]-3,6-diazabicyclo[3.1.1]heptan-3-yl}pyridin-3-yl)pyrazolo[1,5-a]pyridine-3-carbonitrile ()
ARRY-192 ()
SELPERCATINIBARRY-192CT-LX292LOXO-292LOXO292 ()
LY-3527723 ()
LY3527723 ()
RET INHIBITOR LOXO-292 ()
RETEVMO ()
RETSEVMO ()
Retsevmo ()
P&D ID
PD098096
CAS
2152628-33-4
2361241-23-6
Tags
available
drug
Approved by
PMDA
FDA
EMA
First approval
2020
Drug Status
approved
investigational
Max Phase
4.0
Drug indication
non-small cell lung carcinoma
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
Selpercatinib (LOXO-292) is a potent, selective RET kinase inhibitor with IC50 values of 14.0 nM, 24.1 nM, and 530.7 nM for RET (WT), RET (V804M), and RET (G810R), respectively. Selpercatinib has anticancer activity[1][2].
PRICE
83
DESCRIPTION
Selpercatinib (LOXO-292) is a potent, selective and orally bioavailable ATP-competitive RET kinase inhibitor that was developed by Loxo Oncology. It inhibits wild-type RET, RET fusions,and RET carrying activating mutations and acquired resistance mutations . This reference by Subbiah et al. contains preclinical and proof-of-concept data for LOXO-292. This compound was rationally designed to offer a novel therapeutic option for heavily pretreated, multikinase inhibitor-experienced patients whose tumours carry diverse RET alterations.
(GtoPdb)
DESCRIPTION
On May 2020 FDA approved selpercatinib to treat lung and thyroid cancers.
(PKIDB)
DESCRIPTION
Selpercatinib (LOXO-292) is a tyrosine kinase inhibitor with antineoplastic properties, displaying IC50 values of 14.0 nM for RET (WT), 24.1 nM for RET (V804M), and 530.7 nM for RET (G810R).
(TargetMol Bioactive Compound Library)
[[ p.pathway_name ]]
[[ compound.targets[tid].gene_name ]]
Cell lines
1
Organisms
0
Compound Sets
18
AdooQ Bioactive Compound Library
Axon Medchem Screening Library
Cayman Chemical Bioactives
ChEMBL Approved Drugs
ChEMBL Drugs
DrugBank
DrugBank Approved Drugs
DrugCentral
DrugCentral Approved Drugs
EU-OPENSCREEN Bioactive Compound Library
Guide to Pharmacology
MedChem Express Bioactive Compound Library
NCATS Inxight Approved Drugs
NIH Approved Oncology Drugs
PKIDB
ReFrame library
Selleckchem Bioactive Compound Library
TargetMol Bioactive Compound Library
[[ a.name ]]
[[ ligand_id ]]
free of charge
External IDs
21
Molecular Weight
525.25
Hydrogen Bond Acceptors
10
Hydrogen Bond Donors
1
Rotatable Bonds
8
Ring Count
7
Aromatic Ring Count
4
cLogP
3.28
TPSA
112.04
Fraction CSP3
0.38
Chiral centers
2.0
Largest ring
6.0
QED
0.37
Structural alerts
0
No structural alerts detected
Related compounds
Custom attributes
(extracted from source data)
Target
RET
RET inhibitor
c-RET
Pathway
Protein Tyrosine Kinase/RTK
Apoptosis
Tyrosine Kinase/Adaptors
Source data
