General
Preferred name
RUXOLITINIB
Synonyms
RUXOLITINIB PHOSPHATE ()
INCB-18424 ()
Ruxolitinib (sulfate) ()
INCB018424 sulfate ()
INCB-018424, Jakafi, Ruxolitinib Phosphate, INCB-018424 Salt ()
INCB018424 phosphate ()
INCB018424 ()
INC424 ()
INC 424 phosphate ()
(R)-Ruxolitinib ()
Ruxolitinib (INCB-18424) phosphate ()
INCB 018424 phosphate ()
INCB018424(R)-Ruxolitinib ()
INCB018424 (Ruxolitinib) ()
Jakafi ()
CTP-543 ()
Ruxolitinib (phosphate) ()
INC-424 ()
INCB-018424 ()
JAKAVI ()
Ruxolitinib (INCB018424) ()
DEURUXOLITINIB ()
DEURUXOLITINIB PHOSPHATE ()
INCB18424 ()
INCB018424, INC424 ()
Ruxolitinib sulfate ()
Ruxolitinib monophosphate ()
Ruxolitinib (as phosphate) ()
INCB-018424 Salt ()
INCB-18424 PHOSPHATE ()
INCB-018424 PHOSPHATE ()
INCB018424 PHOSPHATE ()
INCB018424 SALT ()
Opzelura ()
C-21543 ()
D8-ruxolitinib ()
D8- ruxolitinib phosphate ()
C-21543 phosphate ()
D8-ruxolitinib phosphate ()
CTP-543 phosphate ()
P&D ID
PD003424
CAS
941678-49-5
1092939-17-7
1092939-15-5
1513883-39-0
1092939-16-6
Tags
probe
covalent binder
drug
natural product
drug candidate
available
Approved by
EMA
FDA
First approval
2011
Drug Status
investigational
approved
Drug indication
Pancreatic cancer
Vitiligo
Alopecia
Nasopharyngeal carcinoma
Essential thrombocythemia
Coronavirus Disease 2019 (COVID-19)
Atopic dermatitis
High-risk myelofibrosis
Max Phase
Phase 4
Phase 3
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)
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)
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 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 inhibitor of Janus kinases 1 and 2 (Informer Set)
DESCRIPTION Potent VEGFR, PDGFR and FGFR inhibitor (Tocris Bioactive Compound Library)
DESCRIPTION Potent and selective beta-secretase (BACE) inhibitor (Tocris 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)
Cell lines
7
Organisms
2
Compound Sets
43
AdooQ Bioactive Compound Library
A11041
Axon Medchem Screening Library
1598
BOC Sciences Bioactive Compounds
ruxolitinib-sulfate-cas-1092939-16-6-item-84-456890
Cayman Chemical Bioactives
11609
23215
ChEMBL Approved Drugs
CHEMBL1789941
CHEMBL1795071
ChEMBL Drugs
CHEMBL1789941
CHEMBL1795071
CHEMBL4594381
CHEMBL4594382
Chemical Probes.org
ruxolitinib
Clinical kinase drugs
Concise Guide to Pharmacology 2017/18
5688
Concise Guide to Pharmacology 2019/20
5688
Concise Guide to Pharmacology 2021/22
5688
Concise Guide to Pharmacology 2023/24
5688
CovalentInDB
CI006053
Drug Repurposing Hub
DrugBank
DB08877
DrugBank Approved Drugs
DB08877
DrugCentral
4190
DrugCentral Approved Drugs
4190
DrugMAP
DM20KYR
DM7Q98D
DMNORK8
DMBT46Y
DrugMAP Approved Drugs
DM7Q98D
EU-OPENSCREEN Bioactive Compound Library
EOS101294
Guide to Pharmacology
5688
11410
High-quality chemical probes
PD003424
Informer Set
639450
JUMP-MOA Compound Set
25126798
JUMP-Target 1 Compound Set
25126798
Kinase Inhibitors (best-in-class)
LINCS compound set
10138-101
10138-105
10138-999
LSP-MoA library (Laboratory of Systems Pharmacology)
CHEMBL1789941
CHEMBL1795071
LSP-OptimalKinase library (Laboratory of Systems Pharmacology)
CHEMBL1789941
CHEMBL1795071
Mcule NIBR MoA Box Subset
MCULE-9293763455
MedChem Express Bioactive Compound Library
HY-50856
HY-50858
NCATS Inxight Approved Drugs
82S8X8XX8H
NIH Approved Oncology Drugs
Novartis Chemogenetic Library (NIBR MoA Box)
PKIDB
ReFrame library
Selleckchem Bioactive Compound Library
INCB18424
ruxolitinib-phosphate
TargetMol Bioactive Compound Library
T1829
T3043
Tocris Bioactive Compound Library
7064
7048
Tool Compound Set
Welcome Trust Cancer Drugs
206
ZINC Tool Compounds
ZINC000043207851
External IDs
76
Properties
(calculated by RDKit )
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
TYK2
JAK1, JAK2, JAK3, TYK2
JAK1/2 inhibitor
Mitophagy
Apoptosis related,Autophagy,JAK,Mitophagy
JAK1, JAK2
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
Source data