NSC 319726

Alias: NSC319726; NSC-319726; NSC 319726
Cat No.:V0017 Purity: ≥98%
NSC319726 is a novel and potent p53(R175) mutant reactivator with with potential anticancer activity.
NSC 319726 Chemical Structure CAS No.: 71555-25-4
Product category: p53
This product is for research use only, not for human use. We do not sell to patients.
Size Price Stock Qty
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25mg
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Purity & Quality Control Documentation

Purity: ≥98%

Product Description

NSC319726 is a novel and potent p53(R175) mutant reactivator with with potential anticancer activity. It exhibits growth inhibition in cells expressing mutant p53 (IC50 for p53(R175) mutant is 8 nM), but it has no effect on p53 wild-type cells.

Biological Activity I Assay Protocols (From Reference)
Targets
R175 (p53 = 8 nM)
ln Vitro
NSC319726 is a p53(R175) mutant reactivator, exhibits growth inhibition in cells expressing mutant p53, with an IC50 for p53(R175) mutant of 8 nM, showing no inhibition for p53 wild-type cells, and exhibiting selectivity of 10- to 100-fold over other hotspot p53 mutants. p53(R175)-dependent apoptosis is induced by NSC319276. The p53(R175) mutant protein undergoes a conformational change similar to that of the WT after being treated with NSC319726, which restores sequence-specific p53 transcription. NSC319726's ability to chelate zinc ions and undergo redox changes are both necessary for the compound to be active. [1]
ln Vivo
NSC319726 (5mg/kg, 7days) exhibits greater toxicity for p53(R172H/R172H) mice, with only 30% survival, as opposed 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]
Enzyme Assay
After two days of serial compound dilution treatment, 5,000 TOV112D cells (5,000 cells/well, in a 100 ml culture) are cultured in a 96-well plate and reach a confluence of 50% to 60%. Following a 3-day incubation period, the growth is assessed using the MTS reagent and a Victor Plate reader instrument.
Cell Assay
Viability assays are done. The cells are cultured in a 12-well plate at a density of 5×104 cells per well in a 1 ml of culture, and are treated with serial dilutions of the compound on the second day to reach a confluence of 50% to 60%. Guava ViaCount reagent and Guava PCA instrument are used to measure the growth after three days of incubation.
Animal Protocol
5-10 mg/kg/day, up to 7 days
DMSO
p53+/+, p53-/- and p53R172H knockin mice
References

[1]. Cancer Cell . 2012 May 15;21(5):614-625.

These protocols are for reference only. InvivoChem does not independently validate these methods.
Physicochemical Properties
Molecular Formula
C11H14N4S
Molecular Weight
234.32
Exact Mass
234.0939
Elemental Analysis
C, 56.38; H, 6.02; N, 23.91; S, 13.68
CAS #
71555-25-4
Appearance
Solid powder
SMILES
C/C(=N\NC(=S)N1CCC1)/C2=CC=CC=N2
InChi Key
XDHBUMNIQRLHGO-UKTHLTGXSA-N
InChi Code
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+
Chemical Name
N-[(E)-1-pyridin-2-ylethylideneamino]azetidine-1-carbothioamide
Synonyms
NSC319726; NSC-319726; NSC 319726
HS Tariff Code
2934.99.9001
Storage

Powder      -20°C    3 years

                     4°C     2 years

In solvent   -80°C    6 months

                  -20°C    1 month

Shipping Condition
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
Solubility Data
Solubility (In Vitro)
DMSO: ~19 mg/mL (~81.1 mM)
Water: <1 mg/mL (slightly soluble or insoluble)
Ethanol: <1 mg/mL
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

*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.

Calculator

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An example of molarity calculation using the molarity calculator is shown below:
What is the mass of compound required to make a 10 mM stock solution in 5 ml of DMSO given that the molecular weight of the compound is 350.26 g/mol?
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Dilution Calculator allows you to calculate how to dilute a stock solution of known concentrations. For example, you may Enter C1, C2 & V2 to calculate V1, as detailed below:

What volume of a given 10 mM stock solution is required to make 25 ml of a 25 μM solution?
Using the equation C1V1 = C2V2, where C1=10 mM, C2=25 μM, V2=25 ml and V1 is the unknown:
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g/mol

Molecular Weight Calculator allows you to calculate the molar mass and elemental composition of a compound, as detailed below:

Note: Chemical formula is case sensitive: C12H18N3O4  c12h18n3o4
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In vivo Formulation Calculator (Clear solution)
Step 1: Enter information below (Recommended: An additional animal to make allowance for loss during the experiment)
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Calculation results

Working concentration mg/mL;

Method for preparing DMSO stock solution mg drug pre-dissolved in μL DMSO (stock solution 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 stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O,mix and clarify.

(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
             (2) Be sure to add the solvent(s) in order.

Biological Data
  • A “WT-like” conformational change in the p53-175 mutant protein induced by NSC319726. Cancer Cell . 2012 May 15;21(5):614-625.
  • Restoration of site-specific p53-175 mutant protein transactivational function by NSC319726. Cancer Cell . 2012 May 15;21(5):614-625.
  • In vivo evidence of NSC319726 mediated p53-175 mutant reactivation. Cancer Cell . 2012 May 15;21(5):614-625.
  • Zinc ion chelation and redox changes are important for the NSC319726 mediated p53-175 mutant reactivation. Cancer Cell . 2012 May 15;21(5):614-625.
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