General
Preferred name
MOMELOTINIB
Synonyms
Momelotinib Mesylate ()
CYT387 (Mesylate) ()
CYT-387, Momelotinib Dihydrochloride, CYT-11387, GS-0387 ()
CYT387 ()
CYT11387 ()
LM-1149 ()
CYT 387 ()
Momelotinib (sulfate) ()
CYT387 Mesylate ()
CYT387 sulfate salt ()
CYT387 (sulfate salt) ()
CYT-0387 ()
CYT-11387 ()
CYT-387 ()
GS-0387 ()
jaktinib ()
Momelotinib (CYT387) ()
LM-1149 , CYT11387 ()
CYT387 DIHYDROCHLORIDE ()
CYT-387 DIHYDROCHLORIDE ()
Ojjaara ()
Momelotinib dihydrochloride ()
Momelotinib hydrochloride hydrate ()
Omjjara ()
CYT-387 DIHYDROCHLORIDE MONOHYDRATE ()
CYT-11387 DIHYDROCHLORIDE MONOHYDRATE ()
MOMELOTINIB DIHYDROCHLORIDE MONOHYDRATE ()
P&D ID
PD003635
CAS
1056634-68-4
1056636-06-6
1056636-07-7
Tags
available
drug
Drug indication
Essential thrombocythemia
myeloproliferative disorder
Thrombocythemia
Polycythemia vera
Myelofibrosis
Drug Status
approved
investigational
Max Phase
4.0
First approval
2024
2023
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 Momelotinib (a.k.a. CYT387 and GS0387) is an oral Janus kinase inhibitor (ATP-competitive)/activin A receptor type 1 (ACVR1) inhibitor . Inhibition of JAK1/2 is proposed to improve constitutional symptoms (fatigue, night sweats, bone pain) and splenomegaly in myelofibrosis patients. Momelotinib also inhibits the bone morphogenetic protein kinase ACVR1, a mechanism that improves iron homeostasis and erythropoiesis via down-regulation of hepcidin , and which may provide benefit to combat anaemia/thrombocytopenia in myelofibrosis . (GtoPdb)
DESCRIPTION Momelotinib (CYT387) is an ATP-competitive inhibitor of JAK1/JAK2 with IC50a of 11 nM and 18 nM,respectively. CYT387 shows much less activity against JAK3.
PRICE 88
DESCRIPTION Momelotinib sulfate (CYT387 sulfate salt) is an ATP-competitive inhibitor of JAK1/JAK2 with IC50 of 11 nM/18 nM, 10-fold selectivity versus JAK3 (IC50=155 nM).
DESCRIPTION Jaktinib is a deuterated analogue of . It has also been called gecacitinib . The compound behaves as a dual Janus kinase/ACVR1 inhibitor. (GtoPdb)
DESCRIPTION inhibitor of Janus kinases 1 and 2 (Informer Set)
DESCRIPTION On September 2023, FDA approved Momelotinib to treat intermediate or high-risk myelofibrosis in adults with anemia (PKIDB)
DESCRIPTION Momelotinib (CYT387) is an ATP-competitive inhibitor of JAK1/JAK2. (Enamine Bioactive Compounds)
DESCRIPTION Momelotinib (LM-1149) is an orally bioavailable small-molecule inhibitor of Janus kinases 1 and 2 (JAK1/2) with IC50 of 11 nM/18 nM. JAK1/2 inhibitor CYT387 competes with JAK1/2 for ATP binding, which may result in inhibition of JAK1/2 activation, inhibition of the JAK-STAT signaling pathway, and so the induction of apoptosis and a reduction of tumor cell proliferation in JAK1/2-expressing tumor cells. (TargetMol Bioactive Compound Library)
DESCRIPTION CYT387 sulfate is an ATP-competitive inhibitor of JAK1/JAK2 with IC50 of 11 nM/18 nM, ~10-fold selectivity versus JAK3. (BOC Sciences Bioactive Compounds)
DESCRIPTION CYT387 Mesylate is an ATP-competitive inhibitor of JAK1/JAK2 with IC50 of 11 nM/18 nM, ~10-fold selectivity versus JAK3. (BOC Sciences Bioactive Compounds)
Cell lines
14
Organisms
0
Compound Sets
27
AdooQ Bioactive Compound Library
A10263
Axon Medchem Screening Library
1681
BOC Sciences Bioactive Compounds
cyt387-sulfate-salt-cas-1056636-06-6-item-84-456716
cyt387-mesylate-cas-1056636-07-7-item-84-456717
Cayman Chemical Bioactives
16246
ChEMBL Approved Drugs
CHEMBL1078178
CHEMBL2219411
CHEMBL6068336
ChEMBL Drugs
CHEMBL1078178
CHEMBL2219411
CHEMBL6068336
Clinical kinase drugs
CZ-OPENSCREEN Bioactive Library
Drug Repurposing Hub
DrugBank
DB11763
DrugBank Approved Drugs
DB11763
DrugMAP
DMF98Q0
Enamine Bioactive Compounds
EBC-11462
EU-OPENSCREEN Bioactive Compound Library
EOS100601
EUbOPEN Chemogenomics Library
EUB0000673
Guide to Pharmacology
7791
14393
Informer Set
660429
LINCS compound set
10140-101
10140-114
LSP-MoA library (Laboratory of Systems Pharmacology)
CHEMBL1078178
LSP-OptimalKinase library (Laboratory of Systems Pharmacology)
CHEMBL1078178
MedChem Express Bioactive Compound Library
HY-10961
HY-10962
Novartis Chemogenetic Library (NIBR MoA Box)
PKIDB
ReFrame library
Selleckchem Bioactive Compound Library
Cyt387
TargetMol Bioactive Compound Library
T1849
ZINC Tool Compounds
ZINC000043199890
External IDs
119
Properties
(calculated by RDKit )
Molecular Weight
414.18
Hydrogen Bond Acceptors
7
Hydrogen Bond Donors
2
Rotatable Bonds
6
Ring Count
4
Aromatic Ring Count
3
cLogP
2.98
TPSA
103.17
Fraction CSP3
0.22
Chiral centers
0.0
Largest ring
6.0
QED
0.6
Structural alerts
0
No structural alerts detected
Related compounds
Custom attributes
(extracted from source data)
Target
JAK1
JAK2
JAK
Autophagy
JAK1, JAK2, JAK3
JAK1/2 inhibitor
JAK3
Apoptosis related,Autophagy,JAK
Compound status
clinical
Pathway
Epigenetics
Stem Cell/Wnt
JAK/STAT Signaling
Angiogenesis
Apoptosis
Chromatin/Epigenetic
Stem Cells
Tyrosine Kinase/Adaptors
Protein Tyrosine Kinase/RTK
Targets
JAK1,JAK2
Member status
member
MOA
Jak2 Inhibitors
Jak1 Inhibitors
Tyk2 Inhibitors
JAK inhibitor
Recommended Cell Concentration
None
Source data