Determine the necessary mass, volume, or concentration for preparing a solution.
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| SKU | Size | Availability |
Price | Qty |
|---|---|---|---|---|
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A176692-5mg
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5mg |
3
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$66.90
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A176692-25mg
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25mg |
2
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$232.90
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|
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A176692-100mg
|
100mg |
2
|
$649.90
|
|
Restores mutant p53 activity
| 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. |
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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| 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= |
Find and download the COA for your product by matching the lot number on the packaging.
| Lot Number | Certificate Type | Date | Item |
|---|---|---|---|
| Certificate of Analysis | Jul 29, 2024 | A176692 | |
| Certificate of Analysis | Jul 29, 2024 | A176692 | |
| Certificate of Analysis | May 10, 2024 | A176692 | |
| Certificate of Analysis | May 10, 2024 | A176692 | |
| Certificate of Analysis | May 10, 2024 | A176692 |
| 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 |
Starting at $69.90