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Catalog:
SLK-S7149
Brand:
Selleck
CAS:
71555-25-4
Overview
MDL
MFCD01665446
Molecular Weight
234.32
Molecular Formula
C11H14N4S
SMILES
C(=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 mg
5 mg
10 mg
1 mM
4.2677 mL
21.3383 mL
42.6767 mL
5 mM
0.8535 mL
4.2677 mL
8.5353 mL
10 mM
0.4268 mL
2.1338 mL
4.2677 mL
50 mM
0.0854 mL
0.4268 mL
0.8535 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.
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.