General
Preferred name
MASITINIB
Synonyms
AB1010 ()
AB-1010 mesylate ()
AB-1010 ()
Masitinib ( AB1010) ()
AB 1010 ()
Masitinib (mesylate) ()
KINAVET ()
MASICAN ()
MASITINIB MESILATE ()
Masitinib mesylate ()
MASITINIB METHANESULFONATE ()
MASIVET ()
MASIVIERA ()
Masitinib (AB1010) ()
Masitinib ()
P&D ID
PD003354
CAS
790299-79-5
1048007-93-7
Tags
available
drug
drug candidate
Drug indication
Multiple sclerosis
Gastrointestinal stromal tumour
Metastatic gastric or gastroesophageal junction cancer
Ovarian cancer
Amyotrophic lateral sclerosis
Pancreatic cancer
Drug Status
withdrawn
approved
vet_approved
investigational
Max Phase
4.0
First approval
2008
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
Using the trade name Masivet, this compound has been used for several years to treat mast cell tumours in dogs . It is a receptor tyrosine kinase (RTK) inhibitor, with inhibitory activity at the cKIT, platelet derived growth factor receptor (PDGFR) and fibroblast growth factor receptor (FGFR) RTKs .
SARS-CoV-2: Using X-ray crystallography, masitinib has been shown to bind (non-covalently) into the catalytic site of the SARS-CoV-2 3CL protease (Mpro) , which corresponds with detection of in vitro Mpro inhibitory activity. It does not bind to the other viral protease PLpro. (GtoPdb)
SARS-CoV-2: Using X-ray crystallography, masitinib has been shown to bind (non-covalently) into the catalytic site of the SARS-CoV-2 3CL protease (Mpro) , which corresponds with detection of in vitro Mpro inhibitory activity. It does not bind to the other viral protease PLpro. (GtoPdb)
DESCRIPTION
inhibitor of c-KIT, PDGFRA, and PDGFRB
(Informer Set)
DESCRIPTION
Masitinib mesylate is a novel inhibitor for Kit and PDGFRα/β with IC50 of 200 nM and 540 nM/800 nM, weak inhibition to ABL and c-Fms.
(BOC Sciences Bioactive Compounds)
[[ p.pathway_name ]]
[[ compound.targets[tid].gene_name ]]
Cell lines
1
Organisms
2
Compound Sets
30
AdooQ Bioactive Compound Library
Axon Medchem Screening Library
BOC Sciences Bioactive Compounds
Cayman Chemical Bioactives
ChEMBL Approved Drugs
ChEMBL Drugs
Clinical kinase drugs
Concise Guide to Pharmacology 2017/18
Concise Guide to Pharmacology 2019/20
Concise Guide to Pharmacology 2021/22
Concise Guide to Pharmacology 2023/24
CZ-OPENSCREEN Bioactive Library
Drug Repurposing Hub
DrugBank
DrugBank Approved Drugs
DrugMAP
EU-OPENSCREEN Bioactive Compound Library
Guide to Pharmacology
Informer Set
LSP-MoA library (Laboratory of Systems Pharmacology)
LSP-OptimalKinase library (Laboratory of Systems Pharmacology)
Novartis Chemogenetic Library (NIBR MoA Box)
PKIDB
ReFrame library
Selleckchem Bioactive Compound Library
TargetMol Bioactive Compound Library
Welcome Trust Cancer Drugs
Withdrawn 2.0
[[ a.name ]]
[[ ligand_id ]]
free of charge
External IDs
43
Molecular Weight
498.22
Hydrogen Bond Acceptors
7
Hydrogen Bond Donors
2
Rotatable Bonds
7
Ring Count
5
Aromatic Ring Count
4
cLogP
5.26
TPSA
73.39
Fraction CSP3
0.25
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)
Target
KIT
PDGFRA
PDGFRB
ABL1
c-Fms
Hck
PDGFR??
Lyn B
SRC
FGFR3, KIT, PDGFRA, PDGFRB
KIT/PDGFR inhibitor
c-Kit
FAK
FGFR
PDGFR
FGFR1
FGFR2
FGFR3
c-Kit,PDGFR
Compound status
clinical
Pathway
RTK signaling
Angiogenesis
Tyrosine Kinase/Adaptors
Cytoskeletal Signaling
Chromatin/Epigenetic
Apoptosis
Protein Tyrosine Kinase/RTK
Targets
KIT,PDGFRA,PDGFRB
Member status
member
MOA
Inhibitors of Signal Transduction Pathways
FGFR3 Inhibitors
KIT (C-KIT) Inhibitors
Angiogenesis Inhibitors
KIT inhibitor, PDGFR tyrosine kinase receptor inhibitor, SRC inhibitor
Indication
mastocytoma
ATC
L01XE22
Source data
