General
Preferred name
MASITINIB
Synonyms
AB1010 ()
AB-1010 ()
SB-75 diacetate ()
AB-1010 mesylate ()
Masitinib ( AB1010) ()
AB 1010 ()
Masitinib (mesylate) ()
Masitinib mesylate ()
Masitinib (AB1010) ()
KINAVET ()
MASICAN ()
MASIVET ()
MASIVIERA ()
Masitinib ()
MASITINIB METHANESULFONATE ()
MASITINIB MESILATE ()
P&D ID
PD003354
CAS
790299-79-5
1048007-93-7
Tags
available
drug
drug candidate
Drug indication
Gastrointestinal stromal tumour
Multiple sclerosis
Ovarian cancer
Neoplasm
Amyotrophic lateral sclerosis
Metastatic gastric or gastroesophageal junction cancer
Pancreatic cancer
COVID-19
Drug Status
vet_approved
approved
withdrawn
investigational
Max Phase
2.0
3.0
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
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
Masitinib (AB1010) is a potent, orally bioavailable, and selective inhibitor of c-Kit (IC50=200 nM for human recombinant c-Kit). It also inhibits PDGFR¦Á/¦Â (IC50s=540/800 nM), Lyn (IC50= 510 nM for LynB), Lck, and, to a lesser extent, FGFR3 and FAK. Masitinib (AB1010) has anti-proliferative, pro-apoptotic activity and low toxicity[1][2][4].
PRICE
47
DESCRIPTION
Masitinib mesylate (AB-1010 mesylate) is a potent, orally bioavailable, and selective inhibitor of c-Kit (IC50=200 nM for human recombinant c-Kit). It also inhibits PDGFR¦Á/¦Â (IC50s=540/800 nM), Lyn (IC50= 510 nM for LynB), Lck, and, to a lesser extent, FGFR3 and FAK. Masitinib mesylate (AB-1010 mesylate) has anti-proliferative, pro-apoptotic activity and low toxicity[1][2][4].
PRICE
49
DESCRIPTION
Masitinib mesylate (AB-1010 mesylate) is a selective, orally bioavailable c-Kit inhibitor with an IC50 of 200 nM for human recombinant c-Kit, and IC50 values of 540/800 nM and 510 nM for PDGFR??/?? and LynB, respectively.
DESCRIPTION
inhibitor of c-KIT, PDGFRA, and PDGFRB
(Informer Set)
DESCRIPTION
Masitinib (AB1010) is a tyrosine-kinase inhibitor used in the treatment of mast cell tumors in animals, specifically dogs. Since its introduction in November 2008 it has been distributed under the commercial name Masivet. It has been available in Europe since the second part of 2009. In the USA it is distributed under the name Kinavet and has been available for veterinaries since 2011.
(TargetMol Bioactive Compound Library)
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)
DESCRIPTION
Masitinib mesylate (AB-1010 mesylate) is a selective, orally bioavailable c-Kit inhibitor with an IC50 of 200 nM for human recombinant c-Kit, and IC50 values of 540/800 nM and 510 nM for PDGFRα/β and LynB, respectively.
(TargetMol Bioactive Compound Library)
[[ p.pathway_name ]]
[[ compound.targets[tid].gene_name ]]
Cell lines
2
Organisms
3
Compound Sets
29
AdooQ Bioactive Compound Library
Axon Medchem Screening Library
BOC Sciences Bioactive Compounds
Cayman Chemical Bioactives
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
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
Apoptosis
c-Kit
FAK
FGFR
FGFR3
LCK
Lyn
PDGFR
PDGFRα
PDGFRβ
SRC
FGFR3, KIT, PDGFRA, PDGFRB
KIT/PDGFR inhibitor
c-Kit,PDGFR
FGFR1
FGFR2
ABL1
c-Fms
Hck
Lyn B
Compound status
clinical
Pathway
RTK signaling
Angiogenesis
Cytoskeletal Signaling
Tyrosine Kinase/Adaptors
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
