PRIMA-1 (Synonyms: NSC-281668)

Name: PRIMA-1
Brand: MedChemExpress
SKU: HY-19980A
Rating: 5.0 (2 reviews)

Cat. No.: HY-19980A Purity: ≥98.0%: FAQs
Data Sheet SDS COA Handling Instructions

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PRIMA-1 (NSC-281668) is a mutant p53 reactivator, restores the sensitivity of TP53 mutant-type thyroid cancer cells to the histone methylation inhibitor 3-Deazaneplanocin A.

For research use only. We do not sell to patients.

PRIMA-1 Chemical Structure

CAS No. : 5608-24-2

Size	Price	Stock	Quantity

Free Sample (0.1 - 0.5 mg)		Apply Now
Solid + Solvent (Highly Recommended)
10 mM * 1 mL in DMSO ready for reconstitution	USD 66	In-stock	Estimated Time of Arrival: December 31
Solution
10 mM * 1 mL in DMSO	USD 66	In-stock	Estimated Time of Arrival: December 31
Solid
5 mg	USD 60	In-stock	Estimated Time of Arrival: December 31
10 mg	USD 84	In-stock	Estimated Time of Arrival: December 31
25 mg	USD 180	In-stock	Estimated Time of Arrival: December 31
50 mg	USD 264	In-stock	Estimated Time of Arrival: December 31
100 mg	USD 480	In-stock	Estimated Time of Arrival: December 31
200 mg	USD 864	In-stock	Estimated Time of Arrival: December 31
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Customer Review

Based on 2 publication(s) in Google Scholar

Other Forms of PRIMA-1:

Eprenetapopt In-stock

2 Publications Citing Use of MCE PRIMA-1

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Biological Activity
Protocol
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References
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Description

PRIMA-1 (NSC-281668) is a mutant p53 reactivator, restores the sensitivity of TP53 mutant-type thyroid cancer cells to the histone methylation inhibitor 3-Deazaneplanocin A.

IC₅₀ & Target

p53^[1]

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^[2].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

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^[3].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Molecular Weight

185.22

Formula

C₉H₁₅NO₃

CAS No.

5608-24-2

Appearance

Solid

Color

White to off-white

SMILES

O=C1C(CO)(CO)N2CCC1CC2

Shipping

Room temperature in continental US; may vary elsewhere.

Storage

Powder	-20°C	3 years
	4°C	2 years
In solvent	-80°C	2 years
	-20°C	1 year

Solvent & Solubility

In Vitro:

H₂O : 100 mg/mL (539.90 mM; Need ultrasonic)

DMSO : 50 mg/mL (269.95 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

Preparing
Stock Solutions

Concentration Solvent Mass	1 mg	5 mg	10 mg

1 mM	5.3990 mL	26.9949 mL	53.9898 mL
5 mM	1.0798 mL	5.3990 mL	10.7980 mL
10 mM	0.5399 mL	2.6995 mL	5.3990 mL

View the Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.

* Note: If you choose water as the stock solution, please dilute it to the working solution, then filter and sterilize it with a 0.22 μm filter before use.

Molarity Calculator
Dilution Calculator

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

Concentration _(start) × Volume _(start) = Concentration _(final) × Volume _(final)

This equation is commonly abbreviated as: C₁V₁ = C₂V₂

Concentration _(start)

Volume _(start)

Concentration _(final)

Volume _(final)

In Vivo:

Select the appropriate dissolution method based on your experimental animal and administration route.

For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for in vivo experiments, it is recommended to prepare freshly and use it on the same day.
The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.

Protocol 1

Add each solvent one by one: 10% DMSO 40% PEG300 5% Tween-80 45% Saline
Solubility: ≥ 2.5 mg/mL (13.50 mM); Clear solution

This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.
Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
Protocol 2

Add each solvent one by one: 10% DMSO 90% (20% SBE-β-CD in Saline)
Solubility: ≥ 2.5 mg/mL (13.50 mM); Clear solution

This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.
Preparation of 20% SBE-β-CD in Saline (4°C, storage for one week): 2 g SBE-β-CD powder is dissolved in 10 mL Saline, completely dissolve until clear.
Protocol 3

Add each solvent one by one: 10% DMSO 90% Corn Oil
Solubility: ≥ 2.5 mg/mL (13.50 mM); Clear solution

This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown). If the continuous dosing period exceeds half a month, please choose this protocol carefully.
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 900 μL Corn oil, and mix evenly.

For the following dissolution methods, please prepare the working solution directly. It is recommended to prepare fresh solutions and use them promptly within a short period of time.
The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.

Protocol 1

Add each solvent one by one: PBS
Solubility: 50 mg/mL (269.95 mM); Clear solution; Need ultrasonic

In Vivo Dissolution Calculator

Please enter the basic information of animal experiments:

Dosage

mg/kg

Animal weight
(per animal)

Dosing volume
(per animal)

μL

Number of animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Calculation results:

Working solution concentration: mg/mL

This product has good water solubility, please refer to the measured solubility data in water/PBS/Saline for details.

The concentration of the stock solution you require exceeds the measured solubility. The following solution is for reference only.If necessary, please contact MedChemExpress (MCE).

Purity & Documentation

Purity: ≥98.0%

Select Batch:

Data Sheet (285 KB) SDS (419 KB)

COA (256 KB) HNMR (241 KB)

Handling Instructions (2659 KB)

References

[1]. 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. [Content Brief]

[2]. Zhang Z, et al. Targeting cancer stem cells with p53 modulators. Oncotarget. 2016 Apr 8. [Content Brief]

[3]. Rao CV, et al. Chemopreventive effects of the p53-modulating agents CP-31398 and Prima-1 in tobacco carcinogen-induced lung tumorigenesis in A/J mice. Neoplasia. 2013 Sep;15(9):1018-27. [Content Brief]

Cell Assay ^[2]	A cell viability assay using yellow tetrazolium salt3-(4,5-Dimethylthiazol-2-yl)-2,5-diphenyl-tetrazolium bromide or MTT is utilized to assess the effects of the p53 SMWC on growth of human carcinoma cell lines. Cells are plated in triplicate in 96-well plates at a density of 2.5×10³ cells/well in 100 μL of complete medium. After 24hr incubation in a humidified 5% atmosphere at 37°C, the cells are treated with increasing concentrations of SMWC for an additional 24 hr period and analyzed for cell growth using the MTT assay. Stock solutions (10 mM) of CP-31398 and PRIMA-1 in PBS are diluted in PBS immediately prior to use. The assay is performed as follows: a 12 mM MTT stock solution is prepared by adding 1 mL of sterile PBS to 5 mg MTT and mixing by vortex or sonication until dissolved. Once prepared, the MTT solution is stored for four weeks at 4°C protected from light.A 500 mL SDS-HCl solution consisting of 0.01 M HCl, 10% propanol and 5 gm SDS is prepared by mixing the solution gently by inversion until the SDS dissolved.100 μL of cell culture medium is removed from each well and 10 μL of the 12 mM MTT stock solution added. A negative control consisting of 10 μL of the MTT stock solution added to 100 μL of medium is prepared. The plates are incubated at 37°C for 4hr followed by the addition of 100 μL of the SDS-HCl solution to each well and mixing thoroughly using a pipette. The absorbance of each sample is read at 570 nm in an ELISA plate reader. The inhibitory concentration (IC₄₀) doses are determined using standard procedure^[2]. MCE has not independently confirmed the accuracy of these methods. They are for reference only.
Animal Administration ^[3]	Mice^[3] Female A/J mice at 6 weeks of age are used. At 6 weeks of age, mice are fed control irradiated AIN-76A modified diet. At 7 weeks of age, the mice intended for carcinogen treatment receive a single dose of 10 mol (2.07 mg) NNK/mouse by intraperitoneal injection. All mice are weighed once every 2 weeks until termination of the study. Three weeks after NNK treatment, groups of mice (25 mice/group) are fed control AIN-76A or experimental diets containing 50 or 100 ppm CP-31398 or 150 or 300 ppm PRIMA-1 until termination. Mice are killed by CO₂ asphyxiation followed by cervical dislocation after 17 weeks (10 mice/group) or 34 weeks (15 mice/group) of exposure to test agents. At the time of sacrifice, lungs are lavaged, perfused, and fixed in phosphate-buffered formalin, transferred within 2 days to 70% alcohol, and evaluated under a dissecting microscope for the number of tumors and tumor size. Tumors on the lung surface are enumerated by at least two experienced readers, blinded to sample identifiers, using a dissecting microscope. Tumor diameters are measured using Fisher brand digital calipers. MCE has not independently confirmed the accuracy of these methods. They are for reference only.
References	[1]. 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. [Content Brief] [2]. Zhang Z, et al. Targeting cancer stem cells with p53 modulators. Oncotarget. 2016 Apr 8. [Content Brief] [3]. Rao CV, et al. Chemopreventive effects of the p53-modulating agents CP-31398 and Prima-1 in tobacco carcinogen-induced lung tumorigenesis in A/J mice. Neoplasia. 2013 Sep;15(9):1018-27. [Content Brief]

Complete Stock Solution Preparation Table

Optional Solvent	Concentration Solvent Mass	1 mg	5 mg	10 mg	25 mg

DMSO / H₂O	1 mM	5.3990 mL	26.9949 mL	53.9898 mL	134.9746 mL
	5 mM	1.0798 mL	5.3990 mL	10.7980 mL	26.9949 mL
	10 mM	0.5399 mL	2.6995 mL	5.3990 mL	13.4975 mL
	15 mM	0.3599 mL	1.7997 mL	3.5993 mL	8.9983 mL
	20 mM	0.2699 mL	1.3497 mL	2.6995 mL	6.7487 mL
	25 mM	0.2160 mL	1.0798 mL	2.1596 mL	5.3990 mL
	30 mM	0.1800 mL	0.8998 mL	1.7997 mL	4.4992 mL
	40 mM	0.1350 mL	0.6749 mL	1.3497 mL	3.3744 mL
	50 mM	0.1080 mL	0.5399 mL	1.0798 mL	2.6995 mL
	60 mM	0.0900 mL	0.4499 mL	0.8998 mL	2.2496 mL
	80 mM	0.0675 mL	0.3374 mL	0.6749 mL	1.6872 mL
	100 mM	0.0540 mL	0.2699 mL	0.5399 mL	1.3497 mL

* Note: If you choose water as the stock solution, please dilute it to the working solution, then filter and sterilize it with a 0.22 μm filter before use.

PRIMA-1 Related Classifications

Help & FAQs

Do most proteins show cross-species activity?
Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

PRIMA-15608-24-2NSC-281668PRIMA1PRIMA 1NSC281668NSC 281668AutophagyMDM-2/p53FerroptosisApoptosisInhibitorinhibitorinhibit

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PRIMA-1 (Synonyms: NSC-281668)

Customer Review

Other Forms of PRIMA-1:

PRIMA-1 Related Antibodies

2 Publications Citing Use of MCE PRIMA-1

Featured Recommendations

•Related Screening Libraries:

•Related Small Molecules:

•Related Proteins:

Biological Activity

Protocol

Purity & Documentation

References

Customer Review

PRIMA-1 Related Antibodies

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Complete Stock Solution Preparation Table

PRIMA-1 Related Classifications

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