General
Preferred name
Eprenetapopt
Synonyms
APR-246 ()
PRIMA-1Met ()
Eprenetapopt (APR-246) ()
PRIMA-1 MET ()
Apr 246 ()
P&D ID
PD018455
CAS
5291-32-7
Tags
available
prodrug
drug candidate
Drug indication
Esophageal cancer
Bladder cancer
Myelodysplastic syndrome
Ovarian cancer
Gastric adenocarcinoma
Solid tumour/cancer
Melanoma
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
Eprenetapopt (APR-246) is a first-in-class, small molecule that restores wild-type p53 functions in TP53-mutant cells. Eprenetapopt triggers apoptosis in tumor cells. Eprenetapopt also targets the selenoprotein thioredoxin reductase 1 (TrxR1), a key regulator of cellular redox balance[1][2][3].
PRICE
55
DESCRIPTION
APR-246 is a quinuclidinone derivative that targets the Wrap53 gene with potential antineoplastic activity. This agent may work synergistically with other antineoplastic agents. The Wrap53 transcript, a natural p53 antisense transcript, regulates endogenous p53 mRNA levels and additional induction of p53 protein by targeting the 5' untranslated region of p53 mRNA.
(BOC Sciences Bioactive Compounds)
DESCRIPTION
Eprenetapopt (PRIMA-1Met) restores wild-type conformation and function to mutant p53, and triggers apoptosis in tumor cells. PRIMA-1MET also targets the selenoprotein thioredoxin reductase 1 (TrxR1), a key regulator of cellular redox balance.
(TargetMol Bioactive Compound Library)
DESCRIPTION
Microtubule destabilizer
(Tocris Bioactive Compound Library)
[[ p.pathway_name ]]
[[ compound.targets[tid].gene_name ]]
Compound Sets
12
AdooQ Bioactive Compound Library
BOC Sciences Bioactive Compounds
Cayman Chemical Bioactives
ChEMBL Drugs
CZ-OPENSCREEN Bioactive Library
DrugBank
DrugMAP
MedChem Express Bioactive Compound Library
ReFrame library
Selleckchem Bioactive Compound Library
TargetMol Bioactive Compound Library
Tocris Bioactive Compound Library
[[ a.name ]]
[[ ligand_id ]]
free of charge
External IDs
23
Molecular Weight
199.12
Hydrogen Bond Acceptors
4
Hydrogen Bond Donors
1
Rotatable Bonds
3
Ring Count
3
Aromatic Ring Count
0
cLogP
-0.34
TPSA
49.77
Fraction CSP3
0.9
Chiral centers
1.0
Largest ring
6.0
QED
0.68
Structural alerts
0
No structural alerts detected
Related compounds
Custom attributes
(extracted from source data)
Pathway
Apoptosis
Autophagy
Primary Target
p53
Target
Ferroptosis
MDM-2/p53
Apoptosis related,Autophagy,p53
TrxR1
Solubility
Soluble in water (100 mM), and DMSO (100 mM)
Source data
