General
Preferred name
ilginatinib
Synonyms
NS-018 ()
NS-018 hydrochloride ()
NS-018 maleate ()
Ilginatinib (maleate) ()
Ilginatinib hydrochloride ()
NS-018 (maleate) ()
Ilginatinib maleate ()
P&D ID
PD050459
CAS
1239358-86-1
1354799-87-3
1239358-85-0
Tags
available
drug candidate
obsolete probe
Drug indication
Myelofibrosis
Primary myelofibrosis
Drug Status
investigational
Max Phase
2.0
Probe control
Probe control not defined
Orthogonal probes
0
No orthogonal probes found
Similar probes
0
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)
DESCRIPTION
The chemical structure shown here was rendered from the chemical name provided in . The compound is an inhibitor of Janus kinase 2 (JAK2) and Src family kinases .
DESCRIPTION
Ilginatinib (NS-018) is a potent and highly selective JAK2 inhibitor. It has an ATP-competitive mode of action. The chemical structure shown here was rendered from the chemical name provided in . The inhibits some Src family kinases in addition to JAK2 .
(GtoPdb)
DESCRIPTION
Ilginatinib (NS-018) is a highly active and orally bioavailable JAK2 inhibitor, with an IC50 of 0.72 nM, 46-, 54-, and 31-fold selectivity for JAK2 over JAK1 (IC50, 33 nM), JAK3 (IC50, 39 nM), and Tyk2 (IC50, 22 nM).
PRICE
171
DESCRIPTION
Ilginatinib hydrochloride (NS-018 hydrochloride) is a highly active and orally bioavailable JAK2 inhibitor, with an IC50 of 0.72 nM, 46-, 54-, and 31-fold selectivity for JAK2 over JAK1 (IC50, 33 nM), JAK3 (IC50, 39 nM), and Tyk2 (IC50, 22 nM).
PRICE
227
DESCRIPTION
Ilginatinib maleate (NS-018 maleate) is a highly active and orally bioavailable JAK2 inhibitor, with an IC50 of 0.72 nM, 46-, 54-, and 31-fold selectivity for JAK2 over JAK1 (IC50, 33 nM), JAK3 (IC50, 39 nM), and Tyk2 (IC50, 22 nM).
PRICE
196
DESCRIPTION
NS-018, a selective JAK2 as well as Src family tyrosine kinases inhibitor that could probably induce the apoptosis of tumor cells. It is still under Phase I/II trial against Myelofibrosis. IC50: 470 nM for Ba/F3-JAK2V617F cell.
(BOC Sciences Bioactive Compounds)
DESCRIPTION
Ilginatinib (NS-018) is a highly active, orally bioavailable JAK2 inhibitor.
(TargetMol Bioactive Compound Library)
DESCRIPTION
The hydrochloride salt form of NS-018 which is a selective JAK2 as well as Src family tyrosine kinases inhibitor that could probably induce the apoptosis of tumor cells. It is still under Phase I/II trial against Myelofibrosis. IC50: 470 nM for Ba/F3-JAK2
(BOC Sciences Bioactive Compounds)
DESCRIPTION
Ilginatinib hydrochloride (NS-018 hydrochloride) is a highly active, orally bioavailable JAK2 inhibitor.
(TargetMol Bioactive Compound Library)
DESCRIPTION
Ilginatinib maleate (NS-018 maleate) is a highly active, orally bioavailable inhibitor of JAK2.
(TargetMol Bioactive Compound Library)
[[ p.pathway_name ]]
[[ compound.targets[tid].gene_name ]]
Cell lines
1
Organisms
0
Compound Sets
14
BOC Sciences Bioactive Compounds
ChEMBL 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
Drug Repurposing Hub
DrugBank
DrugMAP
Guide to Pharmacology
Obsolete Compounds
ReFrame library
[[ a.name ]]
[[ ligand_id ]]
free of charge
External IDs
31
Molecular Weight
389.18
Hydrogen Bond Acceptors
7
Hydrogen Bond Donors
2
Rotatable Bonds
6
Ring Count
4
Aromatic Ring Count
4
cLogP
4.33
TPSA
80.55
Fraction CSP3
0.14
Chiral centers
1.0
Largest ring
6.0
QED
0.51
Structural alerts
1
historic compounds (Chemical Probes.org)
Obsolete
Related compounds
Custom attributes
(extracted from source data)
Target
JAK
JAK1
JAK2
JAK3
TYK2
JAK1, JAK2, JAK3, TYK2
MOA
JAK inhibitor
Pathway
Angiogenesis
Chromatin/Epigenetic
JAK/STAT Signaling
Stem Cells
Tyrosine Kinase/Adaptors
Epigenetics
Protein Tyrosine Kinase/RTK
Stem Cell/Wnt
Solubility
DMSO: ≥ 34 mg/mL
DMSO: ≥ 35 mg/mL
Source data
