NSC319726, Mutant p53 Activator

NSC319726 is a potent and selective activator of mutant p53R175 (EC50 ~8 nM in mutant p53 cell lines but with >100-fold selectivity in wild type cells). It has potent growth inhibitory activity in mutant p53 cells, particularly for the p53R175 mutant. Mechanistic studies revealed that NSC319726 restores WT structure and function to the p53R175 mutant. It kills p53R175H knock-in mice with extensive apoptosis and inhibits xenograft tumor growth in a 175-allele-specific mutant p53-dependent manner. This activity depends upon the zinc ion chelating properties of the compound as well as redox changes. NSC319726 is an attractive lead compound for anti-cancer drug development.

Product information

CAS Number: 71555-25-4

Molecular Weight: 234.32

Formula: C11H14N4S

Chemical Name: (E)-N'-(1-(pyridin-2-yl)ethylidene)azetidine-1-carbothiohydrazide

Smiles: C/C(=N\NC(=S)N1CCC1)/C1=CC=CC=N1

InChiKey: XDHBUMNIQRLHGO-UKTHLTGXSA-N

InChi: InChI=1S/C11H14N4S/c1-9(10-5-2-3-6-12-10)13-14-11(16)15-7-4-8-15/h2-3,5-6H,4,7-8H2,1H3,(H,14,16)/b13-9+

Technical Data

Appearance: Solid Power.

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

Solubility: DMSO up to 100 mM

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:

NSC319726 was used at 1 µM in vitro and in cellular assays.

In Vivo:

NSC319726 was administrated by intraperitoneal injection (IP) to mice at 5-10 mg/kg once per day for up to 7 days.

References:

1. Yu X, et al. Allele-specific p53 mutant reactivation. (2012) Cancer Cell. 21(5):614-25.
2. Charlotte Harrison. Anticancer drugs: Reactivating p53. (2012) Nature Reviews Drug Discovery 11, 517.

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