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| SKU | Size | Availability |
Price | Qty |
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A424535-1ml
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1ml |
Available within 8-12 weeks(?)
Production requires sourcing of materials. We appreciate your patience and understanding.
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$69.90
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Restores mutant p53 activity
| Synonyms | APR-246 | 5291-32-7 | PRIMA-1MET | Eprenetapopt | 2-(Hydroxymethyl)-2-(methoxymethyl)-1-azabicyclo[2.2.2]octan-3-one | 2-(Hydroxymethyl)-2-(methoxymethyl)quinuclidin-3-one | APR 246 | Eprenetapopt [USAN] | Z41TGB4080 | 3-Quinuclidinone, 2-(hydroxymethyl)-2-(methoxymethyl)- |
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| Specifications & Purity | 10mM in DMSO |
| 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 -80°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 |
| 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. |
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 |
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| ALogP | -0.1 |
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| Activity Type | Relation | Activity value | Units | Action Type | Journal | PubMed Id | doi | Assay Aladdin ID |
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| Activity Type | Relation | Activity value | Units | Action Type | Journal | PubMed Id | doi | Assay Aladdin ID |
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| Activity Type | Relation | Activity value | Units | Action Type | Journal | PubMed Id | doi | Assay Aladdin ID |
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| Mechanism of Action | Action Type | target ID | Target Name | Target Type | Target Organism | Binding Site Name | References |
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| IUPAC Name | 2-(hydroxymethyl)-2-(methoxymethyl)-1-azabicyclo[2.2.2]octan-3-one |
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| 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= |
| 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 |