General
Preferred name
RUXOLITINIB
Synonyms
RUXOLITINIB PHOSPHATE ()
INCB-18424 ()
Ruxolitinib (sulfate) ()
INCB018424 sulfate ()
INCB-018424, Jakafi, Ruxolitinib Phosphate, INCB-018424 Salt ()
INC424 ()
INCB018424 ()
INC 424 phosphate ()
Ruxolitinib (INCB-18424) phosphate ()
INCB018424 phosphate ()
(R)-Ruxolitinib ()
INCB 018424 phosphate ()
INCB018424(R)-Ruxolitinib ()
INCB018424 (Ruxolitinib) ()
Jakafi ()
CTP-543 ()
Ruxolitinib (INCB018424) ()
Ruxolitinib (phosphate) ()
INCB18424 ()
INCB018424, INC424 ()
Ruxolitinib sulfate ()
DEURUXOLITINIB PHOSPHATE ()
INC-424 ()
INCB-018424 ()
JAKAVI ()
DEURUXOLITINIB ()
Ruxolitinib, s- ()
S-Ruxolitinib ()
INCB018424 SALT ()
INCB-18424 PHOSPHATE ()
Ruxolitinib monophosphate ()
INCB-018424 PHOSPHATE ()
Ruxolitinib (as phosphate) ()
Opzelura ()
INCB018424 PHOSPHATE ()
INCB-018424 Salt ()
C-21543 ()
D8-ruxolitinib ()
Leqselvi ()
D8-ruxolitinib phosphate ()
D8- ruxolitinib phosphate ()
C-21543 phosphate ()
CTP-543 phosphate ()
RUXOLITINIB, S- ()
P&D ID
PD003424
CAS
941678-49-5
1092939-17-7
1092939-15-5
1513883-39-0
1092939-16-6
Tags
available
covalent binder
drug
probe
Approved by
EMA
FDA
First approval
2011
2024
Drug indication
Nasopharyngeal carcinoma
Primary myelofibrosis
Pancreatic cancer
Essential thrombocythemia
Atopic dermatitis
High-risk myelofibrosis
Vitiligo
Coronavirus Disease 2019 (COVID-19)
alopecia areata
Neoplasm
Alopecia
Drug Status
approved
investigational
Max Phase
4.0
3.0
Probe info
Probe type
calculated probe
experimental probe
Probe sources
Probe targets
[[ compound.targets[t].gene_name ]]
Probe control
Probe control not defined
Orthogonal probes
41
No orthogonal probes found
Similar probes
2
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)
ABSORPTION
Absorption is rapid and is not affected by food. ; Cmax, 15 mg, healthy subject = 649 nmol/L; ; Tmax, 15 mg, healthy subject = 1.5 hours;; Ruxolitinib does not accumulate significantly. ;
DESCPRITION
a kinase inhibitor, inhibits Janus Associated Kinases (JAKs) JAK1 and JAK2 which mediate the signaling of a number of cytokines and growth factors that are important for hematopoiesis and immune function
COMMENT
This compound inhibits JAK1 IC50 7 nM (1 mM ATP) and JAK2 IC50 9 nM (1 mM ATP) equally well. Because either JAK1 or JAK2 can be a part of any receptor pairing in any in vitro or in vivo setting, this probe evaluates the effect of pan-JAK inhibition. Jun 16 2016 - 5:22pm; Jun 16 2016 - 5:24pm; Validation for this compound is high. No significant inhibtion was observed in a panel of 26 kinases when tested at a concentration 100-fold higher than the IC50 observed for JAK1/2, though the modest selectivity against TYK2 is worth noting. Aug 29 2016 - 10:45am
DESCRIPTION
Ruxolitinib is a Type-1 kinase inhibitor and was first approved by the US FDA in 2011. Ruxolitinib has high potency against Janus kinases 1 and 2 (JAK1, JAK2), as well as against the related family member, tyrosine kinase 2 (TYK2) . Inhibitory activity against JAK3 is only slightly reduced compared to the other three family kinases.
Marketed formulations may contain ruxolitinib phosphate (PubChem CID 25127112). (GtoPdb)
Marketed formulations may contain ruxolitinib phosphate (PubChem CID 25127112). (GtoPdb)
DESCRIPTION
Ruxolitinib (INCB18424) is an orally active and selective JAK1/2 inhibitor with IC50s of 3.3 nM and 2.8 nM in cell-free assays, and has 130-fold selectivity for JAK1/2 over JAK3[1]. Ruxolitinib induces autophagy and kills tumor cells through toxic mitophagy[3].
PRICE
56
DESCRIPTION
Ruxolitinib phosphate (INCB018424 phosphate) is a potent JAK1/2 inhibitor with IC50s of 3.3 nM/2.8 nM, respectively, showing more than 130-fold selectivity over JAK3.
PRICE
53
DESCRIPTION
Deuruxolitinib (CTP-543) is a deuterium-modified analogue of the JAK inhibitor . It is an oral inhibitor that inhibits JAK1/2. The chemical structure, and its use in hair loss disorders are claimed in patent WO2017192905A1 .
(GtoPdb)
MOA
Inhibitor
(Chemical Probes.org)
DESCRIPTION
inhibitor of Janus kinases 1 and 2
(Informer Set)
DESCRIPTION
Treatment of intermediate or high-risk myelofibrosis, including primary myelofibrosis, post-polycythemia vera (post-PV) myelofibrosis and post-essential thrombocythemia (post-ET) myelofibrosis. [Lexicomp] Myeolofibrosis is the proliferation of abnormal bone marrow stem cells which cause fibrosis (the excessive formation of connective tissue).
(PKIDB)
DESCRIPTION
Potent and selective beta-secretase (BACE) inhibitor
(Tocris Bioactive Compound Library)
DESCRIPTION
Ruxolitinib is an antineoplastic agent that inhibits cell proliferation, induces apoptosis of malignant cells, and reduces pro-inflammatory cytokine plasma levels by inhibiting JAK-induced phosphorylation of signal transducer and activator of transcription (STAT). It is used to treat various types of myelofibrosis, polycythemia vera.
(Enamine Bioactive Compounds)
DESCRIPTION
Ruxolitinib (INCB018424) is a JAK1/2 inhibitor (IC50=3.3/2.8 nM) that is potent and selective. Rixolitinib exhibits antitumor activity and induces autophagy and apoptosis.
(TargetMol Bioactive Compound Library)
DESCRIPTION
Potent VEGFR, PDGFR and FGFR inhibitor
(Tocris Bioactive Compound Library)
DESCRIPTION
Ruxolitinib phosphate (INCB18424 phosphate) is a JAK1/2 inhibitor with IC50 of 3.3 nM/2.8 nM. Its selectivity for JAK1/2 is more than 130 times that of JAK3.
(TargetMol Bioactive Compound Library)
DESCRIPTION
Ruxolitinib sulfate (INCB018424) is the first potent, selective, JAK1/2 inhibitor to enter the clinic with IC50 of 3.3 nM/2.8 nM, >130-fold selectivity for JAK1/2 versus JAK3.
(BOC Sciences Bioactive Compounds)
[[ p.pathway_name ]]
[[ compound.targets[tid].gene_name ]]
Cell lines
7
Organisms
2
Compound Sets
46
AdooQ Bioactive Compound Library
Axon Medchem Screening Library
BOC Sciences Bioactive Compounds
ChEMBL Approved Drugs
ChEMBL Drugs
Chemical Probes.org
Clinical kinase drugs
Concise Guide to Pharmacology 2017/18
Concise Guide to Pharmacology 2019/20
Concise Guide to Pharmacology 2021/22
Concise Guide to Pharmacology 2023/24
CovalentInDB
CZ-OPENSCREEN Bioactive Library
Drug Repurposing Hub
DrugBank Approved Drugs
DrugCentral
DrugCentral Approved Drugs
DrugMAP Approved Drugs
Enamine Bioactive Compounds
EU-OPENSCREEN Bioactive Compound Library
EUbOPEN Chemogenomics Library
High-quality chemical probes
Informer Set
JUMP-MOA Compound Set
JUMP-Target 1 Compound Set
Kinase Inhibitors (best-in-class)
LSP-MoA library (Laboratory of Systems Pharmacology)
LSP-OptimalKinase library (Laboratory of Systems Pharmacology)
Mcule NIBR MoA Box Subset
NCATS Inxight Approved Drugs
NIH Approved Oncology Drugs
Novartis Chemogenetic Library (NIBR MoA Box)
PKIDB
ReFrame library
Selleckchem Bioactive Compound Library
Tool Compound Set
Welcome Trust Cancer Drugs
ZINC Tool Compounds
[[ a.name ]]
[[ ligand_id ]]
free of charge
External IDs
85
Molecular Weight
306.16
Hydrogen Bond Acceptors
5
Hydrogen Bond Donors
1
Rotatable Bonds
4
Ring Count
4
Aromatic Ring Count
3
cLogP
3.47
TPSA
83.18
Fraction CSP3
0.41
Chiral centers
1.0
Largest ring
6.0
QED
0.8
Structural alerts
0
No structural alerts detected
Related compounds
Custom attributes
(extracted from source data)
Target
JAK1
JAK2
Tyrosine-protein kinase JAK2
JAK1, JAK2, TYK2
JAK
Autophagy
Tyrosine-protein kinase JAK1
JAK1, JAK2, JAK3, TYK2
JAK1/2 inhibitor
Mitophagy
Apoptosis related,Autophagy,JAK,Mitophagy
JAK1, JAK2
TYK2
Compound status
FDA
Kinase group
TK
Pathway
Epigenetics
Stem Cell/Wnt
JAK/STAT Signaling
Angiogenesis
Chromatin/Epigenetic
Stem Cells
Tyrosine Kinase/Adaptors
Apoptosis
Protein Tyrosine Kinase/RTK
Targets
JAK1,JAK2
Primary Target
JAK Kinase
MOA
Inhibitor
JAK tyrosine kinase inhibitor
JAK inhibitor
Member status
virtual
Indication
myelofibrosis, polycythemia vera
Disease Area
hematologic malignancy, hematology
Target class
Protein kinase
Kinase, Kinase
Orthogonal probe
Baricitinib
Therapeutic Class
Antiviral Agents
Target subclass
TK, TK
Recommended Cell Concentration
None
Source data
