NSC 319726

Catalog No.S7149

For research use only.

NSC319726 is a p53(R175) mutant reactivator, exhibits growth inhibition in cells expressing mutant p53, with IC50 of 8 nM for p53(R175) mutant, shows no inhibition for p53 wild-type cells.

NSC 319726 Chemical Structure

CAS No. 71555-25-4

Selleck's NSC 319726 has been cited by 5 Publications

Purity & Quality Control

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Biological Activity

Description NSC319726 is a p53(R175) mutant reactivator, exhibits growth inhibition in cells expressing mutant p53, with IC50 of 8 nM for p53(R175) mutant, shows no inhibition for p53 wild-type cells.
Features An allele-specific p53 mutant reactivator.
Targets
p53 (R175) [1]
()
8 nM
In vitro

NSC319726 is a p53(R175) mutant reactivator, exhibits growth inhibition in cells expressing mutant p53, with IC50 of 8 nM for p53(R175) mutant, shows no inhibition for p53 wild-type cells, shows 10- to 100-fold selectivity over the other hotspot p53 mutants. NSC319276 induces p53(R175)-mutant-dependent apoptosis. NSC319726 treatment induces a WT-like conformational change in the p53(R175) mutant protein that restores sequence-specific p53 transcription. The activity of NSC319726 depends on the zinc ion chelating properties of the compound as well as redox changes. [1]

In vivo NSC319726 (5mg/kg, 7days) exhibits greater toxicity for p53(R172H/R172H) mice, with only 30% survival, as compared to 100% survival for p53+/+ and p53-/- mice. NSC319726 inhibits the growth of TOV112D-p53(R175H) xenografts, but not H460 (p53+/+) and MDAMB468-p53(R273W) xenografts. [1]

Protocol (from reference)

Kinase Assay:[1]
  • MTS:

    5,000 cells of TOV112D cells (5,000 cells/well, in 100 ml culture) are cultured in 96-well plate to reach the 50%–60% confluence on the second day when treated with serial dilutions of the compounds. The growth is measured by MTS reagent and Victor Plate reader instrument after incubation for 3 days.

Cell Research:[1]
  • Cell lines: MEF with p53 mutations
  • Concentrations: ~10 μM
  • Incubation Time: 3 days
  • Method: Viability assays are done. The cells (5×104 cells/well, in 1 ml culture) are cultured in a 12-well plate to reach the 50%–60% confluence on the second day when treated with serial dilutions of the compound. The growth is measured by Guava ViaCount reagent and Guava PCA instrument after incubation for 3 days.
Animal Research:[1]
  • Animal Models: p53+/+, p53-/- and p53R172H knockin mice
  • Dosages: 5-10 mg/kg/day, up to 7 days
  • Administration: i.p.

Solubility (25°C)

In vitro

DMSO 19 mg/mL
(81.08 mM)
Water Insoluble
Ethanol Insoluble

Chemical Information

Molecular Weight 234.32
Formula

C11H14N4S

CAS No. 71555-25-4
Storage 3 years -20°C powder
2 years -80°C in solvent
Smiles CC(=NNC(=S)N1CCC1)C2=CC=CC=N2

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

Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.

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Tech Support

Answers to questions you may have can be found in the inhibitor handling instructions. Topics include how to prepare stock solutions, how to store inhibitors, and issues that need special attention for cell-based assays and animal experiments.

Handling Instructions

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