General
Preferred name
SARACATINIB
Synonyms
AZD-0530,KIN001-045 ()
AZD0530 ()
AZ-10353926, Saracatinib Difumarate, AZD-0530 difumarate, AZD-0530 ()
Saracatinib (AZD0530) ()
AZD 0530 difumarate ()
Saracatinib (difumarate) ()
AZD0530 (difumarate) ()
SARACATINIB DIFUMARATE ()
AZ-10353926 ()
AZD-0530 ()
AZD-0530 DIFUMARATE ()
Saracatinib fumarate ()
AZD0530 DIFUMARATE ()
P&D ID
PD003218
CAS
379231-04-6
893428-72-3
Tags
available
drug candidate
obsolete probe
Drug indication
Hematologic tumour
Osteosarcoma
Solid tumour/cancer
Drug Status
investigational
Max Phase
3.0
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 Saracatinib was developed as an inhibitor of Src family tyrosine kinases. This compound is now included in AstaZeneca's Open Innovation Pharmacology Toolbox.
Note that some bioactivity data may be associated with the difumarate salt (PubChem CID 44195703).
Saracatinib (AZD0530) is compound 33 in . (GtoPdb)
DESCRIPTION Saracatinib (AZD0530) is a potent Src family inhibitor with IC50s of 2.7 to 11 nM for c-Src, Lck, c-YES, Lyn, Fyn, Fgr, and Blk. Saracatinib shows high selectivity over other tyrosine kinases[1].
PRICE 61
DESCRIPTION Saracatinib (AZD0530) difumarate is a potent Src inhibitor with IC50 values of 2.7-11 nM for c-Src, Lck, c-YES, Lyn, Fyn, Fgr and Blk, and is selective for other tyrosine kinases. [1].
DESCRIPTION inhibitor of SRC and ABL1 (Informer Set)
DESCRIPTION Highly potent and selective HDAC2 inhibitor (Tocris Bioactive Compound Library)
DESCRIPTION Saracatinib (AZD0530) (AZD0530) is an effective Src inhibitor (IC50: 2.7 nM), and effective to Lck, Fyn, Lyn, Blk, Fgr and c-Yes. (TargetMol Bioactive Compound Library)
DESCRIPTION Saracatinib Difumarate is a tyrosine kinase inhibitor selectively targeting Src and Abl, which are commonly overexpressed in chronic myeloid leukema cells. (BOC Sciences Bioactive Compounds)
Cell lines
193
Organisms
6
Compound Sets
26
AdooQ Bioactive Compound Library
A10108
Axon Medchem Screening Library
3284
1456
BOC Sciences Bioactive Compounds
saracatinib-difumarate-cas-893428-72-3-item-454347
Cayman Chemical Bioactives
11497
ChEMBL Drugs
CHEMBL217092
CHEMBL2105677
Clinical kinase drugs
CZ-OPENSCREEN Bioactive Library
Drug Repurposing Hub
DrugBank
DB11805
DrugMAP
DMBLHGP
EUbOPEN Chemogenomics Library
EUB0000662
Guide to Pharmacology
7731
Informer Set
606035
Kinase Inhibitors (best-in-class)
LINCS compound set
10032-101
LSP-MoA library (Laboratory of Systems Pharmacology)
CHEMBL217092
LSP-OptimalKinase library (Laboratory of Systems Pharmacology)
CHEMBL217092
MedChem Express Bioactive Compound Library
HY-10234
HY-10234A
Novartis Chemogenetic Library (NIBR MoA Box)
Obsolete Compounds
saracatinib
PKIDB
ReFrame library
Selleckchem Bioactive Compound Library
AZD0530
TargetMol Bioactive Compound Library
T6078
Tocris Bioactive Compound Library
7189
Welcome Trust Cancer Drugs
38
External IDs
47
Properties
(calculated by RDKit )
Molecular Weight
541.21
Hydrogen Bond Acceptors
10
Hydrogen Bond Donors
1
Rotatable Bonds
8
Ring Count
6
Aromatic Ring Count
3
cLogP
3.94
TPSA
90.44
Fraction CSP3
0.48
Chiral centers
0.0
Largest ring
6.0
QED
0.45
Structural alerts
1
historic compounds (Chemical Probes.org)
Obsolete
Related compounds
Custom attributes
(extracted from source data)
Target
ABL1
SRC
SRC, ABL1
ABL1, LCK, SRC, YES1
Src-Abl inhibitor
Autophagy,EGFR,Src
BLK
c-Src
c-YES
EGFR (L858R)
EGFR (L861Q)
FGR
Fyn
LCK
Lyn
Compound status
clinical
Pathway
ABL signaling
Angiogenesis
Autophagy
JAK/STAT Signaling
Tyrosine Kinase/Adaptors
Protein Tyrosine Kinase/RTK
Known off targets
LCK, c-YES, Lyn, Fyn, FGR, BLK, v-Abl
Kinase group
TK
Primary Target
Src Kinases
MOA
BTK
c-Kit
EGFR
Src
Inhibitor
Src Kinase Inhibitors
Inhibitors of Signal Transduction Pathways
Abl Kinase Inhibitors
Src inhibitor
Member status
virtual
Therapeutic Class
Anticancer Agents
Recommended Cell Concentration
None
Source data