Home Apoptosis p53 activator PRIMA-1

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PRIMA-1 p53 activator

Cat.No.S7723

PRIMA-1 (2,2-Bis(hydroxymethyl)-3-quinuclidinone) is a mutant p53 reactivator. It induces apoptosis and inhibits growth of human tumors with mutant p53.
PRIMA-1 p53 activator Chemical Structure

Chemical Structure

Molecular Weight: 185.22

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Chemical Information, Storage & Stability

Molecular Weight 185.22 Formula

C9H15NO3

 Storage (From the date of receipt)
CAS No. 5608-24-2 Download SDF Storage of Stock Solutions

Synonyms 2,2-Bis(hydroxymethyl)-3-quinuclidinone Smiles C1CN2CCC1C(=O)C2(CO)CO

Solubility

In vitro
Batch:

DMSO : 37 mg/mL (199.76 mM)
(Moisture-contaminated DMSO may reduce solubility. Use fresh, anhydrous DMSO.)

Water : 37 mg/mL

Ethanol : 37 mg/mL

Molarity Calculator

Mass Concentration Volume Molecular Weight

In vivo
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In vivo Formulation Calculator (Clear solution)

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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 addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O, mix and clarify.

Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.

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Mechanism of Action

Targets/IC50/Ki
Mutant p53 [1]
In vitro

PRIMA-1 is converted to compounds that form adducts with thiols in mutant p53. Modification of thiol groups in mutant p53 by this compound's conversion products is sufficient to restore its tumor suppressor activity.[2]. It inhibits the growth of pancreatic cancer cell lines and induces cell cycle arrest and decreases DNA synthesis. This compound selectively induces apoptosis and cell death in mutant p53-expressing pancreatic cancer cells and also leads to activation of p53-dependent apoptotic pathways. It enhances the cytotoxicity of chemotherapeutic agents active against mutant p53 pancreatic cancer cells[1]. This chemical has antileukemic properties in acute promyelocytic leukemia-derived NB4 cells. PRIMA-1-triggered apoptosis is in a dose-dependent and time-dependent manner as indicated by the MTT assay and annexin-V staining. Apoptosis induction by this agent is associated with caspase-9, caspase-7 activation and PARP cleavage. It does not show any significant apoptotic effect in normal human peripheral blood mononuclear cells[4].
In vivo

Intravenous (i.v.) injections of PRIMA-1 in mice does not cause any obvious changes in weight or behavior compared with untreated animals. This compound has in vivo antitumor activity in this animal tumor model. It suppresses in vivo tumor growth in a mutant p53-dependent manner[3].
References

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