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NSC 319726

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NSC 319726
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Cat #: V0017 CAS #: 71555-25-4 Purity ≥ 98%

Description: NSC319726 is a novel and potent p53(R175) mutant reactivator with with potential anticancer activity.

References: Yu X, et al. Allele-specific p53 mutant reactivation. Cancer Cell. 2012 May 15;21(5):614-25.

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Molecular Weight (MW)234.32
Molecular FormulaC11H14N4S
CAS No.71555-25-4
Storage-20℃ for 3 years in powder formr
-80℃ for 2 years in solvent
Solubility In VitroDMSO: 19 mg/mL (81.08 mM)r
Water:<1 mg/mL (slightly soluble or insoluble)r
Ethanol: <1 mg/mL
SMILES CodeC/C(C1=CC=CC=N1)=N\NC(N2CCC2)=S
SynonymsNSC319726; NSC-319726; NSC 319726
ProtocolIn VitroFor NSC319726, the effect was even greater as the IC50 for the 175 mutant was 8 nM while the IC50 of the WT was not reached. NSC319726 did not induce WT p53 protein levels or transcriptional activity as common cytotoxic agents such as etoposide do in vitro. NSC319726 exhibited a much higher sensitivity for the MEF-p53R172H/R172H cell line as compared to the p53+/+ and p53-/- controls. NSC319726 treatment of a MEF cell line derived from p53R172H/R172H mice resulted in a loss of PAB240 immunoflouresence staining.
In VivoAt a dose of 1mg/kg, tumor growth of the H460 (p53+/+) and MDAMB468 (p53R273W) xenografts was not inhibited relative to the vehicle control whereas tumor growth was significantly inhibited in the TOV112D (p53R175H) xenografts. When we lowered the dose ten-fold to 0.1 mg/kg in the TOV112D mice, we observed only a small difference in tumor growth inhibition demonstrating both a dosage effect of the drug and a larger therapeutic window.Taken together, these findings provide in vivo evidence for allele specific p53 mutant reactivation.
These protocols are for reference only. InvivoChem does not independently validate these methods.
Preparing Stock Solutions
Solvent volume to be added Mass (the weight of a compound)
Mother liquor concentration 1mg5mg10mg20mg
1mM4.2677 mL21.3383 mL42.6767 mL85.3534 mL
5mM0.8535 mL4.2677 mL8.5353 mL17.0707 mL
10mM0.4268 mL2.1338 mL4.2677 mL8.5353 mL
20mM0.2134 mL1.0669 mL2.1338 mL4.2677 mL
Quality Control Documentation
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The dilution calculator equation
Concentration(start) × Volume(start) = Concentration(final) × Volume(final)

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Dosage mg/kg Average weight of animals g Dosing volume per animal µL Number of animals
Step Two: Enter the in vivo formulation
%DMSO + % + %Tween 80 + %ddH2O
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Working concentration: mg/ml;
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 add µL PEG300, mix and clarify, next add µL Tween 80,mix and clarify, next add µL ddH2O,mix and clarify.
Note:
  • (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.