PRIMA-1 | CAS 5608-24-2

PRIMA-1

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Size	Price	Stock
250mg	$629	Check With Us
500mg	$899	Check With Us
1g	$1345	Check With Us

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Cat #: V2658 CAS #: 5608-24-2 Purity ≥ 98%

Description: PRIMA-1 [also known as Prima-1; chemcial name, 2,2-Bis(hydroxymethyl)-3-quinuclidinone], a novel and potent small molecule compound which is the active form of APR-246 (also known as PRIMA-1MET), is a mutant p53 reactivator which induces apoptosis and inhibits growth of human tumors.

References: Cui B, et al. PRIMA-1, a mutant p53 reactivator, restores the sensitivity of TP53 mutant-type thyroid cancer cells to the histone methylation inhibitor 3-Deazaneplanocin A. J Clin Endocrinol Metab. 2014 Jun;99(6):E962-70.

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Physicochemical and Storage Information
Protocol
Related Biological Data
Stock Solution Preparation
Quality Control Documentation

Molecular Weight (MW)	185.22
Molecular Formula	C9H15NO3
CAS No.	5608-24-2
Storage	-20℃ for 3 years in powder formr
Storage	-80℃ for 2 years in solvent
Solubility In Vitro	DMSO: 37 mg/mL (199.8 mM)r
	Water: 37 mg/mL (199.8 mM)r
	Ethanol: N/A
Solubility In Vivo	Prima 1; Prima1; Prima-1
SMILES Code	O=C1C(CO)(CO)N2CCC1CC2
Synonyms	2,2-Bis(hydroxymethyl)-3-quinuclidinone

Protocol	In Vitro	The cell lines are cultured in the presence of PRIMA-1 (NSC-281668) at 0-140 μM. The IC50s are 35, 40, 50, 50, 60, 70 and 75 μM for PANC-1, HEC-1-B, SUM149, AN 3CA, Ishikawa, Panc02 and MDA-MB-231 cells, respectively.
	In Vivo	PRIMA-1 (Prima-1) is a p53-modulating agent. 150 or 300 ppm PRIMA-1 significantly suppresses (P<0.0001) lung adenocarcinoma formation by 56% and 62%, respectively, after 17 weeks and 39% and 56%, respectively, after 34 weeks. Administration of 150 or 300 ppm PRIMA-1 significantly suppresses NNK-induced total lung adenocarcinoma formation by 57% or 62% (P<0.0001), respectively, after 17 weeks of exposure and by 39% or 56% (P<0.0001), respectively, after 34 weeks of exposure. As with administration of the lower (50 ppm) dose of CP-31398, administration of the lower (150 ppm) dose of PRIMA-1also slightly increases the number of NNK-induced lung adenomas.
	Animal model	SCID mice

These protocols are for reference only. InvivoChem does not independently validate these methods.

Preparing Stock Solutions

Solvent volume to be added	Mass (the weight of a compound)
Mother liquor concentration	1mg	5mg	10mg	20mg
1mM	5.3990 mL	26.9949 mL	53.9898 mL	107.9797 mL
5mM	1.0798 mL	5.3990 mL	10.7980 mL	21.5959 mL
10mM	0.5399 mL	2.6995 mL	5.3990 mL	10.7980 mL
20mM	0.2699 mL	1.3497 mL	2.6995 mL	5.3990 mL

Quality Control Documentation	Select Batch Purity ≥ 98% COA MSDS NMR HPLC

The molarity calculator equation

Mass(g) = Concentration(mol/L) × Volume(L) × Molecular Weight(g/mol)

Mass

Concentration

Volume

Molecular Weight*

The dilution calculator equation

Concentration_(start) × Volume_(start) = Concentration_(final) × Volume_(final)

This equation is commonly abbreviated as: C₁ V₁ = C₂ V₂

Concentration_(start)

Volume_(start)

Concentration_(final)

Volume_(final)

Step One: Enter information below

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

Step Two: Enter the in vivo formulation

%DMSO + % + %Tween 80 + %ddH₂O

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

Note:

(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
(2) Be sure to add the solvent(s) in order.