General
Preferred name
LESTAURTINIB
Synonyms
CEP-701 ()
CEP-701, SP-924, KT-555, SP924, KT-5555, A-1544750, SPM-924, A-154475 ()
KT-5555 ()
A-154475 ()
A-154475.0 ()
KT-555 ()
KT5555 ()
SP-924 ()
SP924 ()
SPM-924 ()
Cep-701 ()
P&D ID
PD019262
CAS
111358-88-4
Tags
available
nuisance
obsolete probe
drug candidate
Drug indication
Acute myeloid leukaemia
Psoriasis vulgaris
Myeloid leukaemia
Drug Status
investigational
Max Phase
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
Lestaurtinib was identified as an inhibitor of the receptor tyrosine kinase (RTK) FLT3 (fms-related tyrosine kinase 3) with activity against leukemia cells in vitro and in vivo . It has activity against other RTKs. A drug repurposing sceen for breast cancer has identified lestaurtinib as a promising agent which appears to sensitise BRCA mutant and wild type breast cancer cells to the effects of the Poly (ADP-ribose) polymerase 1 (PARP1) inhibitor .
(GtoPdb)
[[ p.pathway_name ]]
[[ compound.targets[tid].gene_name ]]
Cell lines
569
Organisms
0
Compound Sets
15
Cayman Chemical Bioactives
ChEMBL Drugs
Clinical kinase drugs
DrugBank
DrugMAP
Guide to Pharmacology
LSP-MoA library (Laboratory of Systems Pharmacology)
LSP-OptimalKinase library (Laboratory of Systems Pharmacology)
MedChem Express Bioactive Compound Library
Nuisance compounds in cellular assays
Obsolete Compounds
PKIDB
Reference compounds for characterizing cellular injury in high-content cellular morphology assays
Welcome Trust Cancer Drugs
[[ a.name ]]
[[ ligand_id ]]
free of charge
External IDs
36
Molecular Weight
439.15
Hydrogen Bond Acceptors
6
Hydrogen Bond Donors
3
Rotatable Bonds
1
Ring Count
8
Aromatic Ring Count
5
cLogP
3.47
TPSA
88.65
Fraction CSP3
0.27
Chiral centers
3.0
Largest ring
7.0
QED
0.37
Structural alerts
2
historic compounds (Chemical Probes.org)
Obsolete
Nonspecific kinase inhibition
Nuisance compounds
Related compounds
Custom attributes
(extracted from source data)
Pathway
RTK signaling
Apoptosis
Epigenetics
JAK/STAT Signaling
Neuronal Signaling
Protein Tyrosine Kinase/RTK
Stem Cell/Wnt
Target
FLT3, JAK2, NTRK1, RET
FLT3
JAK
STAT
Trk Receptor
Targets
JAK2,FLT3,NTRK1
Cellular injury category
Kinase
Therapeutic Class
Anticancer Agents
Source data
