Name: PRIMA-1
Brand: Selleck Chemicals
SKU: S7723
Rating: 5 (8 reviews)

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Quality Control

Purity: >97%

Cited in Nature Medicine for its top-tier quality
COA
NMR
Microanalysis

Why microanalysis?
Datasheet
SDS

97

Related Targets	Bcl-2 Caspase PD-1/PD-L1 Ferroptosis Apoptosis related Synthetic Lethality STAT TNF-alpha Ras KRas
Other p53 Inhibitors	Eprenetapopt (APR-246) CBL0137 Hydrochloride Pifithrin-α (PFTα) Hhydrobromide Pifithrin-μ Serdemetan (JNJ-26854165) RITA NSC 319726 (ZMC1) NSC348884 Tenovin-6 Tenovin-1

Chemical Information, Storage & Stability

Molecular Weight	185.22	Formula	C₉H₁₅NO₃	Storage (From the date of receipt)	3 years-20°Cpowder
CAS No.	5608-24-2	Download SDF		Storage of Stock Solutions	1 year-80°Cin solvent 1 month-20°Cin solvent
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
=	×	×

Dilution Calculator Molecular Weight Calculator

In vivo Batch:
Homogeneous suspension	CMC-NA	≥5mg/ml	Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.
Clear solution	5% DMSO 1 95% Corn oil Validated by Selleck labs. Should you need adjustments to this formulation, contact our sales team for custom testing.	0.452mg/ml (2.44mM)	Taking the 1 mL working solution as an example, add 50 μL of 9.04 mg/ml clear DMSO stock solution to 950 μL of corn oil and mix evenly. The mixed solution should be used immediately for optimal results.
Clear solution	5%DMSO 1 40%PEG300 2 5%Tween80 3 50%ddH2O Validated by Selleck labs. Should you need adjustments to this formulation, contact our sales team for custom testing.	1.850mg/ml (9.99mM)	Taking the 1 mL working solution as an example, add 50 μL of 37 mg/ml clarified DMSO stock solution to 400 μL of PEG300, mix evenly to clarify it; add 50 μL of Tween80 to the above system, mix evenly to clarify; then continue to add 500 μL of ddH2O to adjust the volume to 1 mL. The mixed solution should be used immediately for optimal results.

In vivo Formulation Calculator (Clear solution)

Step 1: Enter information below (Recommended: An additional animal making an allowance for loss during the experiment)

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

Step 2: Enter the in vivo formulation (This is only the calculator, not formulation. Please contact us first if there is no in vivo formulation at the solubility Section.)

% DMSO + % + % Tween 80 + % ddH₂O

%DMSO+ %

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 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.

Note: 1. Please make sure the liquid is clear before adding the next solvent.
2. Be sure to add the solvent(s) in order. You must ensure that the solution obtained, in the previous addition, is a clear solution before proceeding to add the next solvent. Physical methods such as vortex, ultrasound or hot water bath can be used to aid dissolving.

Mechanism of Action

Targets/IC₅₀/Ki	Mutant p53
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 tumour suppressor activity.. 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. This chemical has antileukaemic properties in acute promyelocytic leukaemia-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.
In vivo	Intravenous (i.v.) injections of PRIMA-1 in mice do not cause any obvious changes in weight or behaviour compared with untreated animals. This compound has in vivo antitumour activity in this animal tumour model. It suppresses in vivo tumour growth in a mutant p53-dependent manner.
References	[1] https://pubmed.ncbi.nlm.nih.gov/24838627/ [2] https://pubmed.ncbi.nlm.nih.gov/19411067/ [3] https://pubmed.ncbi.nlm.nih.gov/11875500/ [4] https://pubmed.ncbi.nlm.nih.gov/27548348/

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PRIMA-1 p53 activator

Chemical Structure

Molecular Weight: 185.22