General
Preferred name
INFIGRATINIB
Synonyms
BGJ-398 ()
NVP-BGJ398 ()
KIN001-271 ()
BGJ398 ()
BGJ398 (NVP-BGJ398|Infigratinib) ()
BGJ398 (NVP-BGJ398) ()
NVP-BGJ398 phosphate ()
Infigratinib phosphate ()
MVP-BGJ398 ()
BGJ-398 phosphate ()
NVP-BGJ398 (phosphate) ()
Infigratinib (BGJ398) ()
Infigratinib monophosphate ()
Truseltiq ()
P&D ID
PD003222
CAS
872511-34-7
1310746-10-1
Tags
available
probe
drug
Approved by
FDA
First approval
2021
2019
Drug Status
investigational
approved
Drug indication
Cholangiocarcinoma
Solid tumour/cancer
Max Phase
Phase 4
Probe info
Probe type
calculated probe
experimental probe
Probe sources
Chemical Probes.org
High-quality chemical probes
Tool Compound Set
Probe targets
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 The discovery and synthesis of BGJ-398 is described in , where it is compound 1h. It is an orally bioavailable pan inhibitor of human fibroblast growth factor receptors (FGFRs) with potential antiangiogenic and antineoplastic activities .
COMMENT This probe has single-digit nM potency on FGFR1,2,3 in both in vitro biochemical and cell-based assays. It shows potency against only 76 other kinases assayed with most significant activity on FGFR4 (60 nM) and VEGFR2 (180 nM). Its selectivity against several related kinases remains unknown, however, (e.g. FLT1, CSFR, c-Kit, etc), which leads to some concern. Control of FGFR-driven tumor xenograft seen at doses 5 mg/kg - 30 mg/kg in multiple models. The preferred probe for FGFR4 is BLU9931 (Cancer Discovery, Hagel et al. 2015).  Jun 12 2016 - 3:07am; This compound is a pan FGFR inhibitor in the nM range with other kinases only being inhibited at high (triple digit) nM or low uM in cells. I think this probe is the best so far though, ideally, there would be separate probes for FGFR 1-4.  Jun 12 2016 - 3:08am; This probe is a potent and selective inhibitor of FGFR1/2/3 (though less potent against FGFR4). It acts as an adequate in vitro and in vivo inhibitor tool for these kinases. Jun 12 2016 - 3:09am
DESCRIPTION The discovery and synthesis of infigratinib (BGJ-398) is described in , where it is compound 1h. It is an orally bioavailable, ATP-competitive pan inhibitor of human fibroblast growth factor receptors (FGFRs) with potential antiangiogenic and antineoplastic activities . (GtoPdb)
MOA Inhibitor (Chemical Probes.org)
DESCRIPTION On May 2021, FDA approved infigratinib to treat adults with cholangiocarcinoma whose disease meets certain criteria (PKIDB)
Cell lines
10
Organisms
0
Compound Sets
26
AdooQ Bioactive Compound Library
A11159
Axon Medchem Screening Library
1775
1944
Cayman Chemical Bioactives
19157
ChEMBL Approved Drugs
CHEMBL1852688
CHEMBL1834657
ChEMBL Drugs
CHEMBL1852688
CHEMBL1834657
Chemical Probes.org
bgj-398
Drug Repurposing Hub
DrugBank
DB11886
DrugBank Approved Drugs
DB11886
DrugCentral
5459
DrugCentral Approved Drugs
5459
DrugMAP
DMNKBEC
EU-OPENSCREEN Bioactive Compound Library
EOS101276
Guide to Pharmacology
7877
High-quality chemical probes
PD003222
Kinase Inhibitors (best-in-class)
LINCS compound set
10183-101
LSP-MoA library (Laboratory of Systems Pharmacology)
CHEMBL1834657
LSP-OptimalKinase library (Laboratory of Systems Pharmacology)
CHEMBL1834657
MedChem Express Bioactive Compound Library
HY-13311
HY-13311A
Novartis Chemogenetic Library (NIBR MoA Box)
PKIDB
ReFrame library
Selleckchem Bioactive Compound Library
bgj398-nvp-bgj398
TargetMol Bioactive Compound Library
T1975
Tool Compound Set
External IDs
40
Properties
(calculated by RDKit )
Molecular Weight
559.19
Hydrogen Bond Acceptors
8
Hydrogen Bond Donors
2
Rotatable Bonds
8
Ring Count
4
Aromatic Ring Count
3
cLogP
5.35
TPSA
95.09
Fraction CSP3
0.35
Chiral centers
0.0
Largest ring
6.0
QED
0.38
Structural alerts
0
No structural alerts detected
Related compounds
Custom attributes
(extracted from source data)
Target
Fibroblast growth factor receptor 2
FGFR
Fibroblast growth factor receptor 1
Fibroblast growth factor receptor 3
Fibroblast growth factor receptor 4
FGFR1
FGFR2
FGFR3
FGFR3 (K650E)
FGFR4
FGFR1, FGFR2, FGFR3, FGFR4, KDR
FGFR1, FGFR2, FGFR3, FGFR4
Known off targets
VEGFR2
Kinase group
TK
Pathway
Angiogenesis
Tyrosine Kinase/Adaptors
Apoptosis
Protein Tyrosine Kinase/RTK
Member status
virtual
MOA
pan FGF-R kinase inhibitor
Angiogenesis Inhibitors
FGFR1 Inhibitors
FGFR2 Inhibitors
FGFR3 Inhibitors
FGFR4 Inhibitors
pan-FGFR inhibitor
FGFR inhibitor
Orthogonal probe
AZD4547
Target class
Protein kinase
Kinase, Kinase, Kinase, Kinase
Target subclass
TK, TK, TK, TK
Source data