General
Preferred name
DACTOLISIB
Synonyms
NVP-BEZ235 ()
BEZ235 ()
BEZ-235, NVP-BEZ235, NVP-BEZ235-NX, NVP-BEZ235-ANA, Dactolisib Tosylate ()
BEZ235 (NVP-BEZ235) ()
BEZ 235 ()
NVP-BEZ235\Dactolisib ()
Dactolisib (Tosylate) ()
BEZ-235 ()
NSC-751249 ()
NVP-BEZ-235 ()
NVP-BEZ235-NX ()
RTB-101 ()
RTB101 ()
DACTOLISIB TOSYLATE ()
BEZ235 (Tosylate) ()
NVP-BEZ 235 (Tosylate) ()
BEZ235 Tosylate ()
Dactolisib tosilate ()
NVP-BEZ235-ANA ()
NVP-BEZ235 (hydrochloride) ()
P&D ID
PD003533
CAS
915019-65-7
1028385-31-0
1028385-32-1
2319647-83-9
Tags
available
drug candidate
Drug indication
Solid tumour/cancer
Drug Status
investigational
Max Phase
Phase 3
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
Dactolisib is an orally bioavailable phosphatidylinositol 3-kinase (PI3K) inhibitor with potential antineoplastic activity. It inhibits the α, β, γ and δ PI3K isoforms, and also inhibits mTOR .
DESCRIPTION
Dactolisib is an orally bioavailable dual PI3K/mTOR inhibitor with potential antineoplastic activity. It inhibits all of the PI3K isoforms and in addition, it effectively targets ATR with IC50 of 21 nM in cells .
COVID-19: Dactolisib (as RTB101) is being evaluated as post-exposure prophylaxis for SARS-CoV-2 infection. (GtoPdb)
COVID-19: Dactolisib (as RTB101) is being evaluated as post-exposure prophylaxis for SARS-CoV-2 infection. (GtoPdb)
DESCRIPTION
inhibitor of PI3K and mTOR kinase activity
(Informer Set)
DESCRIPTION
Dactolisib, also known as BEZ235, is an orally bioavailable phosphatidylinositol 3-kinase (PI3K) inhibitor with potential antineoplastic activity. BEZ235 specifically inhibits PIK3 in the PI3K/AKT kinase (or protein kinase B) signaling pathway, which may trigger the translocation of cytosolic Bax to the mitochondrial outer membrane, increasing mitochondrial membrane permeability.
(BOC Sciences Bioactive Compounds)
DESCRIPTION
BEZ235 tosylate is a dual ATP-competitive PI3K and mTOR inhibitor for p110α/γ/δ/β and mTOR(p70S6K) with IC50 of 4 nM /5 nM /7 nM /75 nM /6 nM in cell-free assays, respectively
(BOC Sciences Bioactive Compounds)
[[ p.pathway_name ]]
[[ compound.targets[tid].gene_name ]]
Cell lines
566
Organisms
1
Compound Sets
26
AdooQ Bioactive Compound Library
Axon Medchem Screening Library
BOC Sciences Bioactive Compounds
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
Drug Repurposing Hub
DrugBank
DrugMAP
Enamine BioReference Compounds
EU-OPENSCREEN Bioactive Compound Library
Guide to Pharmacology
Informer Set
LINCS compound set
LSP-MoA library (Laboratory of Systems Pharmacology)
LSP-OptimalKinase library (Laboratory of Systems Pharmacology)
Novartis Chemogenetic Library (NIBR MoA Box)
PKIDB
ReFrame library
TargetMol Bioactive Compound Library
Welcome Trust Cancer Drugs
[[ a.name ]]
[[ ligand_id ]]
free of charge
External IDs
50
Molecular Weight
469.19
Hydrogen Bond Acceptors
6
Hydrogen Bond Donors
0
Rotatable Bonds
3
Ring Count
6
Aromatic Ring Count
6
cLogP
5.89
TPSA
76.5
Fraction CSP3
0.13
Chiral centers
0.0
Largest ring
6.0
QED
0.32
Structural alerts
0
No structural alerts detected
Related compounds
Custom attributes
(extracted from source data)
Target
MTOR
PIK3CA
PIK3CB
PIK3CD
PIK3CG
PI3K (class 1), mTORC1/2
ATR
mTOR (p70S6K)
p110??
p110¦Á
p110¦Ã
p110¦Ä
ATR, MTOR, PIK3CA, PIK3CD, PIK3CG
PI3K/mTOR inhibitor
Compound status
clinical
Pathway
PI3K signaling
DNA Damage/DNA Repair
PI3K/Akt/mTOR signaling
Autophagy
PI3K/Akt/mTOR
Targets
PIK3CA,PIK3CB,PIK3CD,PIK3CG,MTOR
MOA
ATM/ATR
mTOR
PI3K
PI3K inhibitor
mTOR inhibitor
PKB alpha/Akt1 Inhibitors
mTOR inhibitor, PI3K inhibitor
Member status
virtual
Source data
