General
Preferred name
GEDATOLISIB
Synonyms
PKI-587 ()
PF-05212384 ()
PKI-587, PF-05212384 ()
PF 05212384 ()
PKI 587 ()
Gedatolisib (PF-05212384, PKI-587) ()
Gedatolisib (PKI-587) ()
P&D ID
PD016682
CAS
1197160-78-3
Tags
available
drug candidate
Drug indication
Solid tumour/cancer
Drug Status
investigational
Max Phase
3.0
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
Gedatolisib is an orally bioavailable small molecule inhibitor of phosphatidylinositol 3 kinase (PI3K) and mammalian target of rapamycin (mTOR) with potential antineoplastic activity .
(GtoPdb)
DESCRIPTION
MEK1 inhibitor
(Tocris Bioactive Compound Library)
DESCRIPTION
Gedatolisib (PF-05212384, PKI-587) is a highly potent dual inhibitor of PI3Kα, PI3Kγ and mTOR with IC50 of 0.4 nM, 5.4 nM and 1.6 nM, respectively. Phase 2.
(BOC Sciences Bioactive Compounds)
[[ p.pathway_name ]]
[[ compound.targets[tid].gene_name ]]
Cell lines
12
Organisms
0
Compound Sets
25
AdooQ Bioactive Compound Library
Axon Medchem Screening Library
BOC Sciences Bioactive Compounds
Cayman Chemical Bioactives
ChEMBL Drugs
Clinical kinase 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
CZ-OPENSCREEN Bioactive Library
Drug Repurposing Hub
DrugBank
DrugMAP
EU-OPENSCREEN Bioactive Compound Library
Guide to Pharmacology
LSP-MoA library (Laboratory of Systems Pharmacology)
LSP-OptimalKinase library (Laboratory of Systems Pharmacology)
MedChem Express Bioactive Compound Library
Novartis Chemogenetic Library (NIBR MoA Box)
PKIDB
ReFrame library
Selleckchem Bioactive Compound Library
TargetMol Bioactive Compound Library
Tocris Bioactive Compound Library
[[ a.name ]]
[[ ligand_id ]]
free of charge
External IDs
28
Molecular Weight
615.33
Hydrogen Bond Acceptors
10
Hydrogen Bond Donors
2
Rotatable Bonds
7
Ring Count
6
Aromatic Ring Count
3
cLogP
3.02
TPSA
128.29
Fraction CSP3
0.47
Chiral centers
0.0
Largest ring
6.0
QED
0.41
Structural alerts
0
No structural alerts detected
Related compounds
Custom attributes
(extracted from source data)
Targets
PIK3CA,PIK3CG,MTOR
Pathway
PI3K/Akt/mTOR signaling
PI3K/Akt/mTOR
Target
MTOR
PI3K??
PI3K¦Á
PI3K¦Ã
MTOR, PIK3CA
PI3K/mTOR inhibitor
PI3K
PIK3CA
PIK3CB
PIK3CG
PIK3CD
mTOR,PI3K
Primary Target
PI 3-kinase
MOA
Inhibitor
Mammalian Target of Rapamycin (mTOR
FRAP1) Inhibitors
Phosphatidylinositol 3-Kinase alpha (PI3Kalpha) Inhibitors
Phosphatidylinositol 3-Kinase gamma (PI3Kgamma) Inhibitors
mTOR inhibitor, PI3K inhibitor
Member status
member
Source data
