PRIMA-1
Based on 2 publication(s) in Google Scholar
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.
- Purity: 98.0%
- CAS No.: 5608-24-2
- Formula: C9H15NO3
- Molecular Weight:185.22
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Storage:Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 2 years , -20°C, 1 year
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Biological Activity
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Chemical Information
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Solvent & Solubility
- Protocol
- Purity & Documentation
- References
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Help & FAQs
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Apoptosis Compound Library
HY-L003
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Immunology/Inflammation Compound Library
HY-L007
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Anti-Cancer Compound Library
HY-L025
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Autophagy Compound Library
HY-L029
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Anti-Aging Compound Library
HY-L034
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Ferroptosis Compound Library
HY-L051
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Pyroptosis Compound Library
HY-L059
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Glutamine Metabolism Compound Library
HY-L064
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Anti-Pancreatic Cancer Compound Library
HY-L077
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Anti-Blood Cancer Compound Library
HY-L079
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Anti-Cancer Metabolism Compound Library
HY-L083
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Transcription Factor-Targeted Library
HY-L090
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Targeted Diversity Library
HY-L099
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Anti-Colorectal Cancer Compound Library
HY-L103
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Heterocyclic Compound Library
HY-L138
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Cysteine Targeted Covalent Library
HY-L153
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Cell Death Library
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Anti-Hematopathy Compound Library
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Anti-Ovarian Cancer Compound Library
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Bioactive Compound Library Max
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High-Throughput Bioactive Compound Library
HY-L205
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3D Diverse Fragment Library
HY-L903
Publications Citing Use of MedChemExpress (MCE) PRIMA-1
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Biological Activity
p53[1]
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.
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Chemical Information
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CAS No. 5608-24-2
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Appearance Solid
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Molecular Weight 185.22
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Formula C9H15NO3
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Color White to off-white
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SMILES
O=C1C(CO)(CO)N2CCC1CC2
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Synonyms
NSC-281668
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Shipping
Room temperature in continental US; may vary elsewhere.
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Storage
Powder -20°C 3 years 4°C 2 years In solvent -80°C 2 years -20°C 1 year
Publications (2)
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Journal Impact Factor
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Most Recent
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Adv Healthc Mater
Co-Delivery of 131 I and Prima-1 by Self-Assembled CD44-Targeted Nanoparticles for Anaplastic Thyroid Carcinoma Theranostics. [Abstract]2021 Feb;10(3):e2001029. PMID: 33326188 -
Anal Chem
High-Fidelity and Simultaneous Sensing of Endogenous Mutant and Wild p53 Proteins for Precise Cancer Diagnosis and Drug Screening. [Abstract]2021 Jun 8;93(22):8084-8090. PMID: 34034482
Solvent & Solubility
H2O : 100 mg/mL (539.89 mM; Need ultrasonic)
DMSO : 50 mg/mL (269.94 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)
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.
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.
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
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.
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.
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.
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.
Add each solvent one by one: PBS
Solubility: 50 mg/mL (269.94 mM); Clear solution; Need ultrasonic
Please enter the basic information of animal experiments:
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Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Working solution concentration: 0.22 mg/mL
This product has good water solubility, please refer to the measured solubility data in water/PBS/Saline for details.
Protocol
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].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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.
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Purity & Documentation
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Data Sheet (285 KB)
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SDS (419 KB)
- English - EN (419 KB)
- Français - FR (419 KB)
- Deutsch - DE (419 KB)
- Norwegian - NO (419 KB)
- Español - ES (419 KB)
- Swedish - SV (419 KB)
- Italian - IT (419 KB)
- Portuguese - PT (419 KB)
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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]
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.
| Optional Solvent | Concentration Solvent Mass | 1 mg | 5 mg | 10 mg | 25 mg |
|---|---|---|---|---|---|
| DMSO / H2O | 1 mM | 5.3989 mL | 26.9945 mL | 53.9890 mL | 134.9724 mL |
| 5 mM | 1.0798 mL | 5.3989 mL | 10.7978 mL | 26.9945 mL | |
| 10 mM | 0.5399 mL | 2.6994 mL | 5.3989 mL | 13.4972 mL | |
| 15 mM | 0.3599 mL | 1.7996 mL | 3.5993 mL | 8.9982 mL | |
| 20 mM | 0.2699 mL | 1.3497 mL | 2.6994 mL | 6.7486 mL | |
| 25 mM | 0.2160 mL | 1.0798 mL | 2.1596 mL | 5.3989 mL | |
| 30 mM | 0.1800 mL | 0.8998 mL | 1.7996 mL | 4.4991 mL | |
| 40 mM | 0.1350 mL | 0.6749 mL | 1.3497 mL | 3.3743 mL | |
| 50 mM | 0.1080 mL | 0.5399 mL | 1.0798 mL | 2.6994 mL | |
| 60 mM | 0.0900 mL | 0.4499 mL | 0.8998 mL | 2.2495 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.
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