General
Preferred name
NIROGACESTAT
Synonyms
PF-03084014 ()
PF-3084014 ()
PF03084014 ()
PF 03084014 ()
PF 3084014 hydrobromide ()
Nirogacestat (dihydrobromide) ()
PF-3084014 (dihydrobromide) ()
PF-03084014 (dihydrobromide) ()
Nirogacestat (PF-03084014) ()
NIROGACESTAT HYDROBROMIDE ()
PF 3084014 ()
Nirogacestat dihydrobromide ()
PF-03084014-04 ()
Ogsiveo ()
PF-03084014 Hydrobromide ()
P&D ID
PD012628
CAS
1962925-29-6
1290543-63-3
Tags
available
drug
Drug indication
Neoplasm
Alzheimer disease
Desmoid tumour
Solid tumour/cancer
Drug Status
approved
investigational
Max Phase
4.0
First approval
2023
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
Nirogacestat (PF-3084014) is compound 14f in where it is described as a centrally active γ-secretase inhibitor. It is a reversible, non-competitive, and orally bioactive agent. It was proposed an an anti-tumour agent .
PF-3084014 was also reported as an inhibitor of the NOTCH signalling pathway which bolstered its oncology credentials , since NOTCH inhibition promotes cell cycle arrest and induces apoptosis in tumour cells. (GtoPdb)
PF-3084014 was also reported as an inhibitor of the NOTCH signalling pathway which bolstered its oncology credentials , since NOTCH inhibition promotes cell cycle arrest and induces apoptosis in tumour cells. (GtoPdb)
DESCRIPTION
Nirogacestat (PF-3084014) is a reversible, orally bioavailable, noncompetitive, and selective ¦Ã-secretase inhibitor with an IC50 of 6.2 nM. Inhibition of Notch signaling by Nirogacestat while minimizing gastrointestinal toxicity presents a promising approach for research of Notch receptor-dependent cancers[1].
PRICE
130
DESCRIPTION
Nirogacestat (PF 03084014) is a specific ??-secretase inhibitor (IC50: 6.2 nM, in a cell-free assay).
DESCRIPTION
Nirogacestat dihydrobromide (PF-3084014 dihydrobromide) is a reversible, orally bioavailable, noncompetitive, and selective ¦Ã-secretase inhibitor with an IC50 of 6.2 nM. Inhibition of Notch signaling by Nirogacestat dihydrobromide while minimizing gastrointestinal toxicity presents a promising approach for research of Notch receptor-dependent cancers[1].
DESCRIPTION
PF-3084014 is a selective γ-secretase inhibitor (IC50 = 6.2 nM in a cell-free assay). It has been shown to inhibit self-renewal and proliferation of cancer stem cells.
(BOC Sciences Bioactive Compounds)
DESCRIPTION
Nirogacestat (PF 03084014) is a specific γ-secretase inhibitor (IC50: 6.2 nM, in a cell-free assay).
(TargetMol Bioactive Compound Library)
DESCRIPTION
MAP4K4 (HGK) inhibitor; also inhibits MINK and TNIK
(Tocris Bioactive Compound Library)
DESCRIPTION
PF 3084014 is a potent and selective γ-secretase inhibitor (IC50 = 1.2 and 6.2 nM in whole cell and cell-free assays, respectively). It potently reduces Aβ relative to Notch-related endpoints in vitro and in vivo.
(BOC Sciences Bioactive Compounds)
DESCRIPTION
PF-03084014 inhibits the Notch signalling pathway. It contributes totumor suppression in breast, pancreatic carcinoma, hepatocellular carcinoma and progressive desmoid tumors.
(Enamine Bioactive Compounds)
[[ p.pathway_name ]]
[[ compound.targets[tid].gene_name ]]
Compound Sets
17
BOC Sciences Bioactive Compounds
Cayman Chemical Bioactives
ChEMBL Approved Drugs
ChEMBL Drugs
CZ-OPENSCREEN Bioactive Library
Drug Repurposing Hub
DrugBank
DrugBank Approved Drugs
DrugMAP
Enamine Bioactive Compounds
Guide to Pharmacology
Novartis Chemogenetic Library (NIBR MoA Box)
ReFrame library
Selleckchem Bioactive Compound Library
TargetMol Bioactive Compound Library
Tocris Bioactive Compound Library
[[ a.name ]]
[[ ligand_id ]]
free of charge
External IDs
37
Molecular Weight
489.33
Hydrogen Bond Acceptors
5
Hydrogen Bond Donors
3
Rotatable Bonds
10
Ring Count
3
Aromatic Ring Count
2
cLogP
4.79
TPSA
70.98
Fraction CSP3
0.63
Chiral centers
2.0
Largest ring
6.0
QED
0.45
Structural alerts
0
No structural alerts detected
Related compounds
Custom attributes
(extracted from source data)
Target
¦Ã-secretase
Apoptosis
γ secretase
γ-secretase
??secretase
Apoptosis related,Secretase
Primary Target
?-Secretase
MOA
Inhibitor
Apoptosis Inducers
gamma-Secretase Inhibitors
gamma secretase inhibitor
Member status
member
Pathway
Neuroscience
Proteases/Proteasome
Stem Cells
Neuronal Signaling
Stem Cell/Wnt
Solubility
Soluble to <1 mM in water, to 97 mM in DMSO with warming.
Source data
