1. Apoptosis
  2. MDM-2/p53
  3. NSC319726

NSC319726 (Synonyms: ZMC1)

Cat. No.: HY-18634 Purity: 98.07%
Handling Instructions

NSC319726 (ZMC1) is a mutant p53R175 reactivator; inhibits growth of fibroblasts expressing the p53R175 mutation (IC50 = 8 nM); shows no inhibition for p53 wild-type cells.

For research use only. We do not sell to patients.

NSC319726 Chemical Structure

NSC319726 Chemical Structure

CAS No. : 71555-25-4

Size Price Stock Quantity
Solution
10 mM * 1 mL in DMSO USD 73 In-stock
Estimated Time of Arrival: December 31
Solid + Solvent
10 mM * 1 mL
ready for reconstitution
USD 73 In-stock
Estimated Time of Arrival: December 31
Solid
5 mg USD 66 In-stock
Estimated Time of Arrival: December 31
10 mg USD 110 In-stock
Estimated Time of Arrival: December 31
50 mg USD 385 In-stock
Estimated Time of Arrival: December 31
100 mg USD 660 In-stock
Estimated Time of Arrival: December 31
200 mg   Get quote  
500 mg   Get quote  

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Description

NSC319726 (ZMC1) is a mutant p53R175 reactivator; inhibits growth of fibroblasts expressing the p53R175 mutation (IC50 = 8 nM); shows no inhibition for p53 wild-type cells.

IC50 & Target

IC50: 8 nM (mutant p53R175 reactivator)[1].

In Vitro

For 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.

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

In Vivo

At 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.

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

Molecular Weight

234.32

Formula

C11H14N4S

CAS No.
SMILES

C/C(C1=NC=CC=C1)=N\NC(N2CCC2)=S

Shipping

Room temperature in continental US; may vary elsewhere.

Storage
Powder -20°C 3 years
4°C 2 years
In solvent -80°C 6 months
-20°C 1 month
Solvent & Solubility
In Vitro: 

DMSO : 31.25 mg/mL (133.36 mM; Need ultrasonic)

Preparing
Stock Solutions
Concentration Solvent Mass 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
*Please refer to the solubility information to select the appropriate solvent.
In Vivo:
  • 1.

    Add each solvent one by one:  10% DMSO    40% PEG300    5% Tween-80    45% saline

    Solubility: ≥ 2.08 mg/mL (8.88 mM); Clear solution

  • 2.

    Add each solvent one by one:  10% DMSO    90% corn oil

    Solubility: ≥ 2.08 mg/mL (8.88 mM); Clear solution

*All of the co-solvents are available by MCE.
References

Purity: 98.07%

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Product Name:
NSC319726
Cat. No.:
HY-18634
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