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APR-246 - 97%, high purity , Cellular tumor antigen p53 stabiliser, CAS No.5291-32-7, Cellular tumor antigen p53 stabiliser

    Grade & Purity:
  • ≥97%
In stock
Item Number
A176692
Grouped product items
SKU Size
Availability
Price Qty
A176692-5mg
5mg
3
$66.90
A176692-25mg
25mg
2
$232.90
A176692-100mg
100mg
2
$649.90

Restores mutant p53 activity

Basic Description

Synonyms APR 246 | 2-(Hydroxymethyl)-2-(methoxymethyl)-1-azabicyclo[2.2.2]octan-3-one | Eprenetapopt | Z41TGB4080 | 2-(Hydroxymethyl)-2-(methoxymethyl)quinuclidin-3-one | PRIMA-1MET | Eprenetapopt [USAN]
Specifications & Purity ≥97%
Biochemical and Physiological Mechanisms PRIMA-1Met (APR-246) is a re-activator of mutant p53 activity. It′s the methylated, more potent derivative of PRIMA-1. PRIMA-1Met covalently modifies the core domain of mutated p53 restoring the wild-type conformation and activty of p53 in tumor cells, le
Storage Temp Store at -20°C
Shipped In
Ice chest + Ice pads
This product requires cold chain shipping. Ground and other economy services are not available.
Action Type STABILISER
Mechanism of action Cellular tumor antigen p53 stabiliser
Note Wherever possible, you should prepare and use solutions on the same day. However, if you need to make up stock solutions in advance, we recommend that you store the solution as aliquots in tightly sealed vials at -20°C. Generally, these will be useable for up to one month. Before use, and prior to opening the vial we recommend that you allow your product to equilibrate to room temperature for at least 1 hour. Need more advice on solubility, usage and handling? Please visit our frequently asked questions (FAQ) page for more details.
Product Description

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.

Taxonomic Classification

Taxonomy Tree

Kingdom Organic compounds
Superclass Organoheterocyclic compounds
Class Quinuclidines
Subclass Quinuclidones
Intermediate Tree Nodes Not available
Direct Parent Quinuclidones
Alternative Parents Piperidinones  Trialkylamines  Ketones  Dialkyl ethers  Azacyclic compounds  Primary alcohols  Organic oxides  Hydrocarbon derivatives  
Molecular Framework Aliphatic heteropolycyclic compounds
Substituents Quinuclidone - Piperidinone - Piperidine - Ketone - Tertiary amine - Tertiary aliphatic amine - Dialkyl ether - Ether - Azacycle - Organic oxide - Organic oxygen compound - Organooxygen compound - Organonitrogen compound - Organic nitrogen compound - Alcohol - Carbonyl group - Primary alcohol - Hydrocarbon derivative - Amine - Aliphatic heteropolycyclic compound
Description This compound belongs to the class of organic compounds known as quinuclidones. These are compounds containing a quinuclidine moiety which bears a ketone group.
External Descriptors Not available

Product Properties

ALogP -0.1

Associated Targets(Human)

TP53 Tchem Cellular tumor antigen p53 (48468 Activities)
Activity Type Relation Activity value Units Action Type Journal PubMed Id doi Assay Aladdin ID

Associated Targets(non-human)

Hdac6 Histone deacetylase 6 (222 Activities)
Activity Type Relation Activity value Units Action Type Journal PubMed Id doi Assay Aladdin ID
rep Replicase polyprotein 1ab (378 Activities)
Activity Type Relation Activity value Units Action Type Journal PubMed Id doi Assay Aladdin ID

Mechanisms of Action

Mechanism of Action Action Type target ID Target Name Target Type Target Organism Binding Site Name References

Names and Identifiers

Pubchem Sid 504771071
Pubchem Sid Url https://pubchem.ncbi.nlm.nih.gov/substance/504771071
IUPAC Name 2-(hydroxymethyl)-2-(methoxymethyl)-1-azabicyclo[2.2.2]octan-3-one
INCHI InChI=1S/C10H17NO3/c1-14-7-10(6-12)9(13)8-2-4-11(10)5-3-8/h8,12H,2-7H2,1H3
InChIKey BGBNULCRKBVAKL-UHFFFAOYSA-N
Smiles COCC1(C(=O)C2CCN1CC2)CO
Isomeric SMILES COCC1(C(=O)C2CCN1CC2)CO
Molecular Weight 199.25
Reaxy-Rn 1455580
Reaxys-RN_link_address https://www.reaxys.com/reaxys/secured/hopinto.do?context=S&query=IDE.XRN=1455580&ln=

Certificates(CoA,COO,BSE/TSE and Analysis Chart)

C of A & Other Certificates(BSE/TSE, COO):
Analytical Chart:

Find and download the COA for your product by matching the lot number on the packaging.

5 results found

Lot Number Certificate Type Date Item
H2412009 Certificate of Analysis Jul 29, 2024 A176692
H2412010 Certificate of Analysis Jul 29, 2024 A176692
G2121063 Certificate of Analysis May 10, 2024 A176692
G2121064 Certificate of Analysis May 10, 2024 A176692
G2121142 Certificate of Analysis May 10, 2024 A176692

Chemical and Physical Properties

Solubility DMSO : 100 mg/mL (501.88 mM; Need ultrasonic) H2O : 50 mg/mL (250.94 mM; Need ultrasonic)
Molecular Weight 199.250 g/mol
XLogP3 -0.100
Hydrogen Bond Donor Count 1
Hydrogen Bond Acceptor Count 4
Rotatable Bond Count 3
Exact Mass 199.121 Da
Monoisotopic Mass 199.121 Da
Topological Polar Surface Area 49.800 Ų
Heavy Atom Count 14
Formal Charge 0
Complexity 236.000
Isotope Atom Count 0
Defined Atom Stereocenter Count 0
Undefined Atom Stereocenter Count 1
Defined Bond Stereocenter Count 0
Undefined Bond Stereocenter Count 0
The total count of all stereochemical bonds 0
Covalently-Bonded Unit Count 1

Solution Calculators

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