General
Preferred name
FEDRATINIB
Synonyms
TG-101348 ()
TG101348 ()
SAR-302503, TG-101348, TG-101348, TG101348, SAR-302503 ()
SAR 302503 ()
SAR-302503 ()
SAR302503 ()
TG 101348 ()
CT-TG101 ()
T2830 ()
Fedratinib (hydrochloride hydrate) ()
FEDRATINIB HYDROCHLORIDE ()
TG-101348 (hydrochloride hydrate) ()
SAR 302503 (hydrochloride hydrate) ()
Fedratinib (TG101348) ()
Inrebic ()
SAR302503A ()
P&D ID
PD003532
CAS
936091-26-8
1374744-69-0
Tags
available
obsolete probe
drug
Approved by
EMA
FDA
First approval
2019
Drug Status
investigational
approved
Drug indication
Myelofibrosis
Coronavirus Disease 2019 (COVID-19)
Max Phase
Phase 4
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 Fedratinib (TG‑101348) was initially reported as an orally active JAK2-FLT3 kinase inhibitor, with biological activity via JAK2 inhibition . More recently, this compound has been discovered to function, in addition, as a BRD4 (bromodomain) inhibitor . It is suggested that TG‑101348 be termed a dual kinase-bromodomain inhibitor. Fedratinib is been identified and officially approved as an alternative to the JAK1/2 inhibitor for the treatment of primary and secondary myelofibrosis . (GtoPdb)
DESCRIPTION inhibitor of Janus kinase 2 (Informer Set)
DESCRIPTION On august 2019, FDA approved fedratinib to treat adult patients with intermediate-2 or high-risk primary or secondary myelofibrosis (PKIDB)
Cell lines
0
Organisms
1
Compound Sets
33
AdooQ Bioactive Compound Library
A11082
Axon Medchem Screening Library
1588
Cayman Chemical Bioactives
16289
ChEMBL Approved Drugs
CHEMBL1287853
CHEMBL4297216
ChEMBL Drugs
CHEMBL1287853
CHEMBL4297216
Clinical kinase drugs
Concise Guide to Pharmacology 2017/18
5716
Concise Guide to Pharmacology 2019/20
5716
Concise Guide to Pharmacology 2021/22
5716
Concise Guide to Pharmacology 2023/24
5716
Drug Repurposing Hub
DrugBank
DB12500
DrugBank Approved Drugs
DB12500
DrugCentral
5347
DrugCentral Approved Drugs
5347
DrugMAP
DM4ZBK6
DMN1579
DrugMAP Approved Drugs
DM4ZBK6
Guide to Pharmacology
5716
Informer Set
411808
JUMP-Target 1 Compound Set
16722836
LINCS compound set
10141-101
10141-999
LSP-MoA library (Laboratory of Systems Pharmacology)
CHEMBL1287853
LSP-OptimalKinase library (Laboratory of Systems Pharmacology)
CHEMBL1287853
MedChem Express Bioactive Compound Library
HY-10409
HY-10409A
NCATS Inxight Approved Drugs
6L1XP550I6
NIH Approved Oncology Drugs
Novartis Chemogenetic Library (NIBR MoA Box)
Obsolete Compounds
fedratinib
PKIDB
ReFrame library
Selleckchem Bioactive Compound Library
Fedratinib-SAR302503-TG101348
TargetMol Bioactive Compound Library
T1995
Welcome Trust Cancer Drugs
306
External IDs
47
Properties
(calculated by RDKit )
Molecular Weight
524.26
Hydrogen Bond Acceptors
8
Hydrogen Bond Donors
3
Rotatable Bonds
10
Ring Count
4
Aromatic Ring Count
3
cLogP
4.82
TPSA
108.48
Fraction CSP3
0.41
Chiral centers
0.0
Largest ring
6.0
QED
0.35
Structural alerts
1
historic compounds (Chemical Probes.org)
Obsolete
Related compounds
Custom attributes
(extracted from source data)
Target
JAK2
JAK2 (V617F)
RET
FLT3
BRD4, JAK1, JAK2, JAK3, TYK2
JAK2 Inhibitor
BRD4
Apoptosis related,c-RET,FLT3,JAK
Compound status
clinical
Pathway
Angiogenesis
Apoptosis
Chromatin/Epigenetic
Tyrosine Kinase/Adaptors
JAK/STAT Signaling
Stem Cells
Epigenetics
Protein Tyrosine Kinase/RTK
Stem Cell/Wnt
MOA
JAK
c-RET
FLT
Jak2 Inhibitors
Flt3 (FLK2/STK1) Inhibitors
FLT3 inhibitor, JAK inhibitor
Member status
virtual
Indication
myelofibrosis
Therapeutic Class
Antiviral Agents
Source data