Eprenetapopt (APR246; PRIMA-1MET)

This product is for research use only, not for human use. We do not sell to patients.

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Size	Price	Stock
250mg	$620	Check With Us
500mg	$999	Check With Us
1g	$1495	Check With Us

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Cat #: V2651 CAS #: 5291-32-7 Purity ≥ 98%

Description: Eprenetapopt (APR-246; PRIMA-1MET), a methylated derivative of PRIMA-1 and a mutant p53 reactivator, is a novel and potent small molecule compound that is able to restore wild-type conformation and function to mutant p53, and triggers apoptosis in tumor cells.

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

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Physicochemical and Storage Information
Protocol
Related Biological Data
Stock Solution Preparation
Quality Control Documentation

Molecular Weight (MW)	199.25
Molecular Formula	C10H17NO3
CAS No.	5291-32-7
Storage	-20℃ for 3 years in powder formr
Storage	-80℃ for 2 years in solvent
Solubility In Vitro	DMSO: >10mg/mLr
	Water: <1 mg/mLr
	Ethanol: <1 mg/mL
SMILES Code	O=C1C(COC)(CO)N2CCC1CC2
Synonyms	APR-246; Eprenetapopt; APR246; APR 246; PRIMA-1Met.

Protocol	In Vitro	Eprenetapopt inhibits both recombinant TrxR1 in vitro and TrxR1 in cells. Cellular TrxR1 activity is inhibited by Eprenetapopt irrespective of p53 status. Eprenetapopt can directly affect cellular redox status via targeting of TrxR1. Several small molecules have been shown to restore wild-type activity to mutant p53, including CP-31398, PRIMA-1 and Eprenetapopt, MIRA, STIMA, PhiKan-083 and NSC319726. PRIMA-1 and its methylated analog Eprenetapopt promote correct folding of mutant p53, induce cell death by apoptosis, and inhibit tumor growth in mice. Eprenetapopt has also been shown to reactivate mutant forms of the p63 and p73 proteins that share high structural homology with p53.

These protocols are for reference only. InvivoChem does not independently validate these methods.

Preparing Stock Solutions

Solvent volume to be added	Mass (the weight of a compound)
Mother liquor concentration	1mg	5mg	10mg	20mg
1mM	5.0188 mL	25.0941 mL	50.1882 mL	100.3764 mL
5mM	1.0038 mL	5.0188 mL	10.0376 mL	20.0753 mL
10mM	0.5019 mL	2.5094 mL	5.0188 mL	10.0376 mL
20mM	0.2509 mL	1.2547 mL	2.5094 mL	5.0188 mL

Quality Control Documentation	Select Batch Purity ≥ 98% COA MSDS NMR HPLC

The molarity calculator equation

Mass(g) = Concentration(mol/L) × Volume(L) × Molecular Weight(g/mol)

Mass

Concentration

Volume

Molecular Weight*

The dilution calculator equation

Concentration_(start) × Volume_(start) = Concentration_(final) × Volume_(final)

This equation is commonly abbreviated as: C₁ V₁ = C₂ V₂

Concentration_(start)

Volume_(start)

Concentration_(final)

Volume_(final)

Step One: Enter information below

Dosage mg/kg Average weight of animals g Dosing volume per animal µL Number of animals

Step Two: Enter the in vivo formulation

%DMSO + % + %Tween 80 + %ddH₂O

Calculation Results:

Working concentration: mg/ml;

Method for preparing DMSO master liquid: mg drug pre-dissolved in µL DMSO(Master liquid concentration mg/mL) ,Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug.

Method for preparing in vivo formulation: Take µL DMSO master liquid, next add µL PEG300, mix and clarify, next add µL Tween 80,mix and clarify, next add µL ddH₂O,mix and clarify.

Note:

(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
(2) Be sure to add the solvent(s) in order.