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APR-246 (Eprenetapopt)

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

PRIMA-1MET; Eprenetapopt

Size Price Availability Quantity
10mg USD 112.5  USD125 In stock
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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
References

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.

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

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