General
Preferred name
LY-2584702
Synonyms
LY-2584702 (hydrochloride) ()
LY-2584702 (free base) ()
LY-2584702 tosylate salt ()
LY-2584702 free base ()
LY2584702 Tosylate ()
LY 2584702 tosylate ()
LY2584702 ()
LY-2584702 (tosylate salt) ()
LY-2584702 hydrochloride ()
?LY2584702 (tosylate) ()
LY 2584702 ()
P&D ID
PD038909
CAS
1082949-67-4
1082949-68-5
1082948-81-9
Tags
available
drug candidate
Drug indication
Solid tumour/cancer
Drug Status
investigational
Max Phase
1.0
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
LY2584702 is reported as an ATP competitive, selective inhibitor of the p70 ribosomal protein S6 kinase (p70S6K) . p70S6K is a downstream component of the PI3K/Akt/mTOR signalling pathway regulating cell proliferation and survival.
DESCRIPTION
LY2584702 is reported as an ATP competitive, selective inhibitor of the p70 ribosomal protein S6 kinase (p70S6K) . p70S6K is a downstream component of the PI3K/Akt/mTOR signalling pathway which regulates cell proliferation and survival. LY2584702 was originally developed as a potential oncology therapeutic, but the programme was terminated due to a lack of clinical efficacy. Subsequent study has discovered that LY2584702 produces effects that indicate potential efficacy as a therapy for dyslipidemia . In healthy dyslipidemic volunteers LY2584702 dose‐dependently and significantly reduced pasma low‐density lipoprotein cholesterol and triglycerides, whilst leaving high‐density lipoprotein cholesterol levels unchanged. However, metabolism of LY2584702 generates 4-aminopyrazolo[3,4-d]pyrimidine (4-APP; PubChem CID 75420), a compound which may contribute towards the adverse hepatotoxicity associated with LY2584702 exposure. Further determination of the anti-dyslipidemia potential of p70S6K inhibitors could be advanced by the development of non-4-APP forming compounds.
(GtoPdb)
DESCRIPTION
LY2584702 is an orally available inhibitor of p70S6K signaling, with potential antineoplastic activity.
(BOC Sciences Bioactive Compounds)
DESCRIPTION
The hydrochloride salt form of LY2584702 which is a selective ATP competitive inhibitor of p70 S6 kinase. LY2584702 is still under Phase I trial for evaluating its potential anti-tumor effect.IC50: 4 nM (LY2584702).
(BOC Sciences Bioactive Compounds)
[[ p.pathway_name ]]
[[ compound.targets[tid].gene_name ]]
Cell lines
0
Organisms
1
Compound Sets
17
Axon Medchem Screening Library
BOC Sciences Bioactive Compounds
Cayman Chemical Bioactives
ChEMBL Drugs
Clinical kinase drugs
CZ-OPENSCREEN Bioactive Library
Drug Repurposing Hub
DrugBank
DrugMAP
EU-OPENSCREEN Bioactive Compound Library
Guide to Pharmacology
LINCS compound set
MedChem Express Bioactive Compound Library
ReFrame library
Selleckchem Bioactive Compound Library
[[ a.name ]]
[[ ligand_id ]]
free of charge
External IDs
35
Molecular Weight
445.16
Hydrogen Bond Acceptors
6
Hydrogen Bond Donors
1
Rotatable Bonds
3
Ring Count
5
Aromatic Ring Count
4
cLogP
4.3
TPSA
75.52
Fraction CSP3
0.33
Chiral centers
0.0
Largest ring
6.0
QED
0.48
Structural alerts
0
No structural alerts detected
Related compounds
Custom attributes
(extracted from source data)
Target
Ribosomal S6 Kinase (RSK)
mTOR (p70S6K)
p70 S6K
RPS6KB1
S6K1 inhibitor
S6 Kinase
Pathway
MAPK/ERK Pathway
PI3K/Akt/mTOR signaling
MAPK
Targets
RPS6KB1,RPS6KB2
MOA
ribosomal protein inhibitor
Solubility
10 mM in DMSO
Source data
