PRIMA-1

SKU: orb1224660

Description

A specific mutant p53 reactivator that induces apoptosis and enhances chemotherapeutic cytotoxicity in cancer cell lines; is efficacious against myeloma cells with differential p53 genotypes, causes the demethylation of TP73, through DNMT1 depletion, to subsequently enhance UPR; selectively induces apoptosis and cell cycle arrest in p53 mutant cells compared to CAPAN-2 cells.Blood Cancer Phase 2 Clinical.

Research Area

Neuroscience

Key Properties

• CAS Number: 5608-24-2
• MW: 185.2203
• Purity: >98% (HPLC)
• Formula: C₉H₁₅NO₃
• SMILES: O=C1C(CO)(CO)N2CCC1CC2
• Target: MDM2-p53
• Solubility: DMSO: ≥ 44 mg/mL

Bioactivity

• 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.
• 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.

Storage & Handling

• Storage: Storage temperature: -20°C. Stability: ≥ 2 years
• Expiration Date: 12 months from date of receipt.
• Disclaimer: For research use only

Alternative Names

PRIMA 1 | PRIMA1

Quick Database Links

Gene Symbol

MDM2-p53