PRIMA-1

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.

Product information

CAS Number: 5608-24-2

Molecular Weight: 185.22

Formula: C9H15NO3

Synonym:

NSC-281668

Chemical Name: 2, 2-bis(hydroxymethyl)-1-azabicyclo[2.2.2]octan-3-one

Smiles: OCC1(CO)C(=O)C2CCN1CC2

InChiKey: RFBVBRVVOPAAFS-UHFFFAOYSA-N

InChi: InChI=1S/C9H15NO3/c11-5-9(6-12)8(13)7-1-3-10(9)4-2-7/h7,11-12H,1-6H2

Technical Data

Appearance: Solid Power

Purity: ≥98% (or refer to the Certificate of Analysis)

Solubility: DMSO : 50 mg/mL (269.95 mM; Need ultrasonic)

Shipping Condition: Shipped under ambient temperature as non-hazardous chemical or refer to Certificate of Analysis

Storage Condition: Dry, dark and -20 ^oC for 1 year or refer to the Certificate of Analysis.

Shelf Life: ≥360 days if stored properly.

Stock Solution Storage: 0 - 4 ^oC for 1 month or refer to the Certificate of Analysis.

Drug Formulation: To be determined

HS Tariff Code: 382200

How to use

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.

References:

1. Zhang Z, et al. Targeting cancer stem cells with p53 modulators. Oncotarget. 2016 Apr 8.
2. 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.

Products are for research use only. Not for human use.