Free shipping on all orders over $ 500

APR-246 (Eprenetapopt)

Cat. No. M9623
APR-246 (Eprenetapopt) Structure

PRIMA-1MET; Eprenetapopt

Size Price Availability Quantity
10mg USD 112.5  USD125 In stock
Free Delivery on orders over USD 500 Bulk Inquiry?

Quality Control
Biological Activity

APR-246 (Eprenetapopt), also known as PRIMA-1MET, is a quinuclidinone derivative that targets the Wrap53 gene with potential antineoplastic activity. APR-246 (PRIMA-1MET) enhances apoptosis in mutant p53 carrying cells, compared to the p53 null parental cells. Most p53 mutants are in complex with Hsp70 proteins. PRIMA-1MET treatment increases Hsp70 expression and nucleolar translocation, in parallel with the induction of nucleolar accumulation of mutant p53. Several lines of evidence suggest that PRIMA-1MET can also act independently of the p53 status of the cell.

In animal studies, APR-246 (Eprenetapopt) is well tolerated, APR-246 single treatment inhibits tumor growth by 21% in mice bearing the aggressively growing A2780-CP20 tumor xenografts.

Conversion of different model animals based on BSA (Value based on data from FDA Draft Guidelines)
Species Mouse Rat Rabbit Guinea pig Hamster Dog
Weight (kg) 0.02 0.15 1.8 0.4 0.08 10
Body Surface Area (m2) 0.007 0.025 0.15 0.05 0.02 0.5
Km factor 3 6 12 8 5 20
Animal A (mg/kg) = Animal B (mg/kg) multiplied by  Animal B Km
Animal A Km

For example, to modify the dose of Compound A used for a mouse (20 mg/kg) to a dose based on the BSA for a rat, multiply 20 mg/kg by the Km factor for a mouse and then divide by the Km factor for a rat. This calculation results in a rat equivalent dose for Compound A of 10 mg/kg.

Chemical Information
Molecular Weight 199.25
Formula C10H17NO3
CAS Number 5291-32-7
Purity 100.0%
Solubility DMSO ≥ 30 mg/mL
Water ≥ 30 mg/mL
Storage at -20°C

APR-246 overcomes resistance to cisplatin and doxorubicin in ovarian cancer cells
N Mohell, et al. Cell Death Dis. 2015 Jun 18;6(6):e1794. PMID: 26086967.

APR-246/PRIMA-1MET inhibits thioredoxin reductase 1 and converts the enzyme to a dedicated NADPH oxidase
X Peng, et al. Cell Death Dis. 2013 Oct 24;4(10):e881. PMID: 24157875.

PRIMA-1Met/APR-246 induces apoptosis and tumor growth delay in small cell lung cancer expressing mutant p53
Roza Zandi, et al. Clin Cancer Res. 2011 May 1;17(9):2830-41. PMID: 21415220.

PRIMA-1MET induces nucleolar translocation of Epstein-Barr virus-encoded EBNA-5 protein
Gyorgy Stuber, et al. Mol Cancer. 2009 Mar 26;8:23. PMID: 19323829.

Related p53 Products

FL118 is an inhibitor of human survivin expression, activating tumor suppressor p53 as a novel MOA in p53 wild-type cancer cells.


CBL0137 is a metabolically stable curaxin that activates p53 with an EC50 value of 0.37 µM and inhibits NF-κB with an EC50 of 0.47 µM.


PRIMA-1 is a selective re-activator of mutant p53 activity in tumor cells, and an inducer of apoptosis and inhibitor of growth of human tumors with mutant p53.

PhiKan 083 hydrochloride

PhiKan 083 is a p53 stabilizing agent.


MI-773 (SAR405838) is an orally available MDM2 antagonist with Ki of 0.88 nM. Phase 1.

Abmole Inhibitor Catalog 2017

Keywords: APR-246 (Eprenetapopt), PRIMA-1MET; Eprenetapopt supplier, p53, inhibitors

Contact Us

Products are for research use only. Not for human use. We do not sell to patients.
© Copyright 2010-2020 AbMole BioScience. All Rights Reserved.