General
Preferred name
TAMATINIB
Synonyms
R-406 ()
R406 ()
R406 (free base) ()
R-406 besylate ()
R406 (freebase) ()
R 406 ()
R406 free base ()
R940406 ()
P&D ID
PD003501
CAS
841290-80-0
841290-81-1
Tags
available
drug candidate
Drug indication
Solid tumour/cancer
Drug Status
experimental
investigational
Max Phase
2.0
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 Tamatinib (R406) is a potent ATP-competitive (Type I) Syk inhibitor. It is the active form of the prodrug . (GtoPdb)
DESCRIPTION R406 free base is an orally available and competitive Syk/FLT3 inhibitor for ATP binding with a Ki of 30 nM, potently inhibits Syk kinase activity in vitro with an IC50 of 41 nM, measured at an ATP concentration corresponding to its Km value. R406 free base reduces immune complex-mediated inflammation[1]. R406 free base also inhibits Lyn (IC50=63 nM) and Lck (IC50=37 nM)[2].
PRICE 93
DESCRIPTION R406 is an orally available and competitive Syk/FLT3 inhibitor for ATP binding with a Ki of 30 nM, potently inhibits Syk kinase activity in vitro with an IC50 of 41 nM, measured at an ATP concentration corresponding to its Km value. R406 reduces immune complex-mediated inflammation[1]. R406 also inhibits Lyn (IC50=63 nM) and Lck (IC50=37 nM)[2].
PRICE 183
DESCRIPTION inhibitor of spleen tyrosine kinase (Informer Set)
DESCRIPTION R406 free base (R406 (free base)) is a potent Syk inhibitor. (TargetMol Bioactive Compound Library)
DESCRIPTION R406 (R-406 besylate) is an effective Syk inhibitor (IC50: 41 nM) and shows no effects on Lyn. (TargetMol Bioactive Compound Library)
Cell lines
1
Organisms
0
Compound Sets
25
AdooQ Bioactive Compound Library
A10770
A10769
Axon Medchem Screening Library
1674
Cayman Chemical Bioactives
11422
ChEMBL Drugs
CHEMBL475251
Clinical kinase drugs
Concise Guide to Pharmacology 2017/18
5706
Concise Guide to Pharmacology 2019/20
5706
Concise Guide to Pharmacology 2021/22
5706
Concise Guide to Pharmacology 2023/24
5706
CZ-OPENSCREEN Bioactive Library
Drug Repurposing Hub
DrugBank
DB07159
DrugMAP
DMGANIC
EU-OPENSCREEN Bioactive Compound Library
EOS101409
EUbOPEN Chemogenomics Library
EUB0002301
Guide to Pharmacology
5706
Informer Set
417818
LINCS compound set
10040-101
10040-999
LSP-MoA library (Laboratory of Systems Pharmacology)
CHEMBL475251
LSP-OptimalKinase library (Laboratory of Systems Pharmacology)
CHEMBL475251
MedChem Express Bioactive Compound Library
HY-11108
HY-12067
PKIDB
ReFrame library
Selleckchem Bioactive Compound Library
R406(free-base)
R406
TargetMol Bioactive Compound Library
T2467
T6174
External IDs
41
Properties
(calculated by RDKit )
Molecular Weight
470.17
Hydrogen Bond Acceptors
10
Hydrogen Bond Donors
3
Rotatable Bonds
7
Ring Count
4
Aromatic Ring Count
3
cLogP
3.63
TPSA
128.75
Fraction CSP3
0.27
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)
Target
SYK
Apoptosis
FLT3
RET, SYK
Apoptosis related,FLT3,Syk
Compound status
clinical
MOA
Syk
Syk inhibitor
Pathway
Protein Tyrosine Kinase/RTK
Angiogenesis
Tyrosine Kinase/Adaptors
Recommended Cell Concentration
None
Source data