[CAS NO. 71555-25-4]  NSC 319726

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PRODUCTS SPECIFICATIONS [71555-25-4]

Store
Catalog
SLK-S7149
Brand
Selleck
CAS
71555-25-4

DESCRIPTION [71555-25-4]

Overview

MDLMFCD01665446
Molecular Weight234.32
Molecular FormulaC11H14N4S
SMILESC(=NNC(=S)N1CCC1)(C)C2=CC=CC=N2

For research use only.

Storage

3 years,-20°C,powder
1 years,-80°C,in solvent

Shipping

Room temperature shipping(Stability testing shows this product can be shipped without any cooling measures.)

Preparing Stock Solutions

1 mg5 mg10 mg
1 mM4.2677 mL21.3383 mL42.6767 mL
5 mM0.8535 mL4.2677 mL8.5353 mL
10 mM0.4268 mL2.1338 mL4.2677 mL
50 mM0.0854 mL0.4268 mL0.8535 mL

Description

NSC319726 is a mutant reactivator, exhibits growth inhibition in cells expressing mutant p53, with 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.

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.


Synonyms

1-Azetidinecarbothioic acid, 2-[1-(2-pyridinyl)ethylidene]hydrazide
1-Azetidinecarbothioic acid, [1-(2-pyridinyl)ethylidene]hydrazide
1-Azetidinecarbothioic acid 2-[1-(2-pyridinyl)ethylidene]hydrazide
NSC 319726
ZMC 1