General
Preferred name
pexidartinib
Synonyms
PLX-3397 hydrochloride ()
PLX-3397 ()
PLX-3397 (hydrochloride) ()
Pexidartinib (hydrochloride) ()
CML-261 ()
PLX3397 ()
Pexidartinib (PLX3397) ()
PLX-3397 HCL ()
PLX3397 HCl ()
FP-113 ()
Turalio ()
PEXIDARTINIB HYDROCHLORIDE ()
P&D ID
PD012397
CAS
1029044-16-3
2040295-03-0
Tags
available
drug
probe
Approved by
FDA
First approval
2019
Drug indication
Alzheimer disease
Pigmented villonodular synovitis
Tenosynovial giant cell tumour
Neurofibromatosis type 1
Drug Status
approved
investigational
Max Phase
4.0
Probe info
Probe type
experimental probe
Probe sources
Probe targets
[[ compound.targets[t].gene_name ]]
Probe control
Probe control not defined
Orthogonal probes
4
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
Pexidartinib is an orally available, multi-targeted inhibitor of the receptor tyrosine kinases, Fms-related tyrosine kinase 3 (FLT3), stem cell growth factor receptor (KIT) and colony stimulating factor 1 receptor (CSF1R), with potential antineoplastic activity . Pexidartinib is compound P-0181 in patent US7893075 B2 .
It is active against wild type FLT3 and the FLT3 gatekeeper F691L resistance mutant, but its activity is vulnerable to mutations in the FLT3 activation loop . (GtoPdb)
It is active against wild type FLT3 and the FLT3 gatekeeper F691L resistance mutant, but its activity is vulnerable to mutations in the FLT3 activation loop . (GtoPdb)
DESCRIPTION
Pexidartinib is an orally available, investigational multi-targeted inhibitor of the receptor tyrosine kinases, Fms-related tyrosine kinase 3 (FLT3), stem cell growth factor receptor (KIT) and colony stimulating factor 1 receptor (CSF1R), with potential antineoplastic activity . Pexidartinib is compound P-0181 in patent US7893075 B2 .
MOA
Inhibitor
(Chemical Probes.org)
DESCRIPTION
On august 2019, FDA approved pexidartinib to treat adult patients with symptomatic tenosynovial giant cell tumor
(PKIDB)
[[ p.pathway_name ]]
[[ compound.targets[tid].gene_name ]]
Cell lines
6
Organisms
1
Compound Sets
28
AdooQ Bioactive Compound Library
Axon Medchem Screening Library
Cayman Chemical Bioactives
ChEMBL Approved Drugs
ChEMBL Drugs
Chemical Probes.org
Clinical kinase drugs
CZ-OPENSCREEN Bioactive Library
Drug Repurposing Hub
DrugBank
DrugBank Approved Drugs
DrugCentral
DrugCentral Approved Drugs
DrugMAP
DrugMAP Approved Drugs
EU-OPENSCREEN Bioactive Compound Library
EUbOPEN Chemogenomics Library
Guide to Pharmacology
High-quality chemical probes
Mcule NIBR MoA Box Subset
NCATS Inxight Approved Drugs
NIH Approved Oncology Drugs
Novartis Chemogenetic Library (NIBR MoA Box)
PKIDB
ReFrame library
Selleckchem Bioactive Compound Library
TargetMol Bioactive Compound Library
[[ a.name ]]
[[ ligand_id ]]
free of charge
External IDs
39
Molecular Weight
417.1
Hydrogen Bond Acceptors
4
Hydrogen Bond Donors
2
Rotatable Bonds
5
Ring Count
4
Aromatic Ring Count
4
cLogP
5.23
TPSA
66.49
Fraction CSP3
0.15
Chiral centers
0.0
Largest ring
6.0
QED
0.47
Structural alerts
0
No structural alerts detected
Related compounds
Custom attributes
(extracted from source data)
Targets
CSF1R
Pathway
Angiogenesis
Tyrosine Kinase/Adaptors
Apoptosis
Protein Tyrosine Kinase/RTK
Target
KIT
CSF-1R
FLT3
CSF1R, FLT3, KIT
RTK inhibitor
c-Fms
c-Kit
Apoptosis related,c-Kit,CSF-1R,FLT3
Member status
member
MOA
CSF1R inhibitor
tyrosine kinase inhibitor
Target class
Kinase
Target subclass
TK
Recommended Cell Concentration
None
Source data
