General
Preferred name
LUCITANIB
Synonyms
E-3810, AL-3810, CO-3810, S-80881 ()
E-3810 ()
E 3810 dihydrochloride ()
AL3810 ()
Lucitanib (E3810) hydrochloride ()
AL-3810 ()
CO-3810 ()
S 80881 ()
S-80881 ()
S80881 ()
Lucitanib (hydrochloride) ()
P&D ID
PD012591
CAS
1058137-23-7
2108875-91-6
Tags
available
drug candidate
Drug indication
Neoplasm
Solid tumour/cancer
Drug Status
investigational
Max Phase
2.0
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
Lucitanib is an inhibitor of multiple receptor tyrosine kinases that was investigated for anti-angiogenic and anti-tumourigenic efficacy.
(GtoPdb)
DESCRIPTION
Lucitanib (E-3810) is a novel dual inhibitor of VEGFR and FGFR, potently and selectively inhibits VEGFR1, VEGFR2, VEGFR3, FGFR1 and FGFR2 with IC50s of 7 nM, 25 nM, 10 nM, 17.5 nM, and 82.5 nM, respectively[1][2][3].
PRICE
133
DESCRIPTION
Lucitanib, also known as E-3810, is a novel dual inhibitor targeting human vascular endothelial growth factor receptors (VEGFRs) and fibroblast growth factor receptors (FGFRs) with antiangiogenic activity. VEGFR/FGFR dual kinase inhibitor E-3810 inhibits VEGFR-1, -2, -3 and FGFR-1, -2 kinases in the nM range, which may result in the inhibition of tumor angiogenesis and tumor cell proliferation, and the induction of tumor cell death. Both VEGFRs and FGFRs belong to the family of receptor tyrosine kinases that may be upregulated in various tumor cell types.
(BOC Sciences Bioactive Compounds)
DESCRIPTION
Lucitanib (E-3810) is a novel and potent inhibitor of VEGFR and FGFR, selectively targeting VEGFR1, VEGFR2, VEGFR3, FGFR1, and FGFR2 with IC50 values of 7 nM, 25 nM, 10 nM, 17.5 nM, and 82.5 nM, respectively.
(TargetMol Bioactive Compound Library)
[[ p.pathway_name ]]
[[ compound.targets[tid].gene_name ]]
Cell lines
1
Organisms
0
Compound Sets
15
Axon Medchem Screening Library
BOC Sciences Bioactive Compounds
ChEMBL Drugs
Clinical kinase drugs
Drug Repurposing Hub
DrugBank
DrugMAP
EU-OPENSCREEN Bioactive Compound Library
Guide to Pharmacology
MedChem Express Bioactive Compound Library
PKIDB
ReFrame library
Selleckchem Bioactive Compound Library
TargetMol Bioactive Compound Library
[[ a.name ]]
[[ ligand_id ]]
free of charge
External IDs
41
Molecular Weight
443.18
Hydrogen Bond Acceptors
6
Hydrogen Bond Donors
2
Rotatable Bonds
7
Ring Count
5
Aromatic Ring Count
4
cLogP
4.42
TPSA
95.7
Fraction CSP3
0.23
Chiral centers
0.0
Largest ring
6.0
QED
0.44
Structural alerts
0
No structural alerts detected
Related compounds
Custom attributes
(extracted from source data)
Targets
FLT1,KDR,FLT4,FGFR1,FGFR2,FGFR3
Target
FGFR
FGFR1
FGFR2
VEGFR
VEGFR1
VEGFR2
VEGFR3
FGFR1, FLT1, KDR, KIT, PDGFRA, PDGFRB, RET
VEGFR inhibitor
FGFR,VEGFR
FLT1
KDR
FLT4
MOA
FGFR inhibitor, VEGFR inhibitor
Pathway
Protein Tyrosine Kinase/RTK
Angiogenesis
Tyrosine Kinase/Adaptors
Source data
