General
Preferred name
Debio-1347
Synonyms
CH-5183284 ()
CH5183284 ()
FF284 ()
Debio 1347 ()
zoligratinib ()
CH5183284, FF284 ()
CH5183284 (debio-1347) ()
Zoligratinib (Debio-1347) ()
FGFR INHIBITOR DEBIO 1347 ()
P&D ID
PD018312
CAS
1265229-25-1
Tags
available
drug candidate
Drug indication
Breast cancer
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
Zoligratinib (DEBIO1347) is a FGFR1/2/3 inhibitor that is being investigated for antineoplastic activity . The compound is ATP-competitive, potent and orally available.
(GtoPdb)
DESCRIPTION
Zoligratinib (Debio 1347) is an orally available and selective FGFR inhibitor with IC50s of 9.3, 7.6, and 22 nM for FGFR1, FGFR2, FGFR3, and FGFR4, respectively.
PRICE
53
DESCRIPTION
Debio-1347, also known as FF284 and CH5183284, is an orally bioavailable inhibitor of the fibroblast growth factor receptor subtypes 1 (FGFR-1), 2 (FGFR-2) and 3 (FGFR-3), with potential antineoplastic activity. FGFR inhibitor debio 1347 binds to and inhibits FGFR-1, -2, and -3, which result in the inhibition of FGFR-mediated signal transduction pathways. This leads to the inhibition of both tumor cell proliferation and angiogenesis, and causes cell death in FGFR-overexpressing tumor cells. FGFR, a family of receptor tyrosine kinases upregulated in many tumor cell types, is essential for tumor cellular proliferation, differentiation and survival.
(BOC Sciences Bioactive Compounds)
DESCRIPTION
Zoligratinib (CH5183284) is a selective and orally available FGFR inhibitor, which is for FGFR1(IC50=9.3 nM), FGFR2(IC50=7.6 nM), FGFR3(IC50=290), and FGFR4(IC50=22 nM), respectively.
(TargetMol Bioactive Compound Library)
[[ p.pathway_name ]]
[[ compound.targets[tid].gene_name ]]
Cell lines
1
Organisms
0
Compound Sets
14
BOC Sciences Bioactive Compounds
Cayman Chemical Bioactives
ChEMBL Drugs
Clinical kinase drugs
CZ-OPENSCREEN Bioactive Library
Drug Repurposing Hub
DrugBank
DrugMAP
Guide to Pharmacology
LINCS compound set
MedChem Express Bioactive Compound Library
ReFrame library
Selleckchem Bioactive Compound Library
TargetMol Bioactive Compound Library
[[ a.name ]]
[[ ligand_id ]]
free of charge
External IDs
20
Molecular Weight
356.14
Hydrogen Bond Acceptors
5
Hydrogen Bond Donors
3
Rotatable Bonds
3
Ring Count
5
Aromatic Ring Count
5
cLogP
3.35
TPSA
105.38
Fraction CSP3
0.05
Chiral centers
0.0
Largest ring
6.0
QED
0.43
Structural alerts
0
No structural alerts detected
Related compounds
Custom attributes
(extracted from source data)
Targets
FGFR1,FGFR2,FGFR3,FGFR4
Target
FGFR
FGFR1
FGFR2
FGFR3
FGFR4
FGFR1, FGFR2, FGFR3
MOA
fibroblast growth factor inhibitor
Pathway
Protein Tyrosine Kinase/RTK
Angiogenesis
Tyrosine Kinase/Adaptors
Source data
