General
Preferred name
ATIPRIMOD
Synonyms
ATIPRIMOD DIHYDROCHLORIDE ()
atiprimod dimaleate ()
SKF-106615 ()
SK&F-106615 ()
SKF-106615-A2 ()
SK&F-106615-A2 ()
SK&F 106615-A2 ()
SKF-106615-I2 ()
SK&F 106615-12 ()
SK&F 106615-I2 ()
SK&F-106615-I2 ()
P&D ID
PD069964
CAS
130065-61-1
123018-47-3
Tags
available
drug candidate
Drug indication
Multiple myeloma
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
atiprimod is orally bioavailable small molecule belonging to the azaspirane class of cationic amphiphilic agents with anti-inflammatory, antineoplastic, and antiangiogenic properties. Atiprimod inhibits the phosphorylation of signal transducer and activator of transcription 3 (STAT3), blocking the signalling pathways of interleukin-6 and vascular endothelial growth factor (VEGF) and downregulating the anti-apoptotic proteins Bcl-2, Bcl-XL, and Mcl-1, thereby inhibiting cell proliferation, inducing cell cycle arrest, and inducing apoptosis.
(BOC Sciences Bioactive Compounds)
DESCRIPTION
Selective allosteric activator of Lyn kinase
(Tocris Bioactive Compound Library)
DESCRIPTION
Atiprimod dihydrochloride is the dihydrochloride salt form of atiprimod, which is an orally bioavailable small molecule belonging to the azaspirane class of cationic amphiphilic agents. It is a JAK2 inhibitor with IC50 value of 397 nM. It has anti-inflammatory, antineoplastic, and anti-angiogenic activities. It inhibits the phosphorylation of signal transducer and activation of transcription 3 (STAT3) and STAT5. It downregulates the anti-apoptotic proteins Bcl-2, Bcl-XL, and Mcl-1 and blocks the signaling pathways of interleukin-6, vascular endothelial growth factor (VEGF). It also inhibits cell growth, induction of cell cycle arrest, and apoptosis in cells expressing the JAK2V617F mutation.
(BOC Sciences Bioactive Compounds)
[[ p.pathway_name ]]
[[ compound.targets[tid].gene_name ]]
Compound Sets
8
BOC Sciences Bioactive Compounds
ChEMBL Drugs
Drug Repurposing Hub
DrugBank
DrugMAP
DrugMatrix
ReFrame library
Tocris Bioactive Compound Library
[[ a.name ]]
[[ ligand_id ]]
free of charge
External IDs
34
Molecular Weight
336.35
Hydrogen Bond Acceptors
2
Hydrogen Bond Donors
0
Rotatable Bonds
10
Ring Count
2
Aromatic Ring Count
0
cLogP
5.57
TPSA
6.48
Fraction CSP3
1.0
Chiral centers
0.0
Largest ring
6.0
QED
0.51
Structural alerts
0
No structural alerts detected
Related compounds
Custom attributes
(extracted from source data)
Primary Target
JAK Kinase
MOA
Inhibitor
JAK inhibitor, STAT inhibitor
Target
JAK2, STAT3
Source data
