| Size | Price | Stock | Qty |
|---|---|---|---|
| 1mg |
|
||
| 5mg |
|
||
| 10mg |
|
||
| 25mg |
|
||
| 50mg |
|
||
| 100mg |
|
||
| 250mg |
|
||
| 500mg |
|
||
| Other Sizes |
|
Purity: ≥98%
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.
| 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 |
|
|||
| References |
| Molecular Formula |
C11H14N4S
|
|
|---|---|---|
| Molecular Weight |
234.32
|
|
| Exact Mass |
234.093
|
|
| Elemental Analysis |
C, 56.38; H, 6.02; N, 23.91; S, 13.68
|
|
| CAS # |
71555-25-4
|
|
| Related CAS # |
|
|
| PubChem CID |
5351307
|
|
| Appearance |
Off-white to light yellow solid powder
|
|
| Density |
1.3±0.1 g/cm3
|
|
| Boiling Point |
367.7±34.0 °C at 760 mmHg
|
|
| Flash Point |
176.2±25.7 °C
|
|
| Vapour Pressure |
0.0±0.8 mmHg at 25°C
|
|
| Index of Refraction |
1.659
|
|
| LogP |
0.17
|
|
| Hydrogen Bond Donor Count |
1
|
|
| Hydrogen Bond Acceptor Count |
3
|
|
| Rotatable Bond Count |
2
|
|
| Heavy Atom Count |
16
|
|
| Complexity |
286
|
|
| Defined Atom Stereocenter Count |
0
|
|
| SMILES |
S=C(N([H])/N=C(\C([H])([H])[H])/C1=C([H])C([H])=C([H])C([H])=N1)N1C([H])([H])C([H])([H])C1([H])[H]
|
|
| 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 |
|
|
| 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 (In Vitro) |
|
|||
|---|---|---|---|---|
| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.08 mg/mL (8.88 mM) (saturation unknown) in 10% DMSO + 40% PEG300 + 5% Tween80 + 45% Saline (add these co-solvents sequentially from left to right, and one by one), clear solution.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 20.8 mg/mL clear DMSO stock solution to 400 μL PEG300 and mix evenly; then add 50 μL Tween-80 to the above solution and mix evenly; then add 450 μL normal saline to adjust the volume to 1 mL. Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH₂ O to obtain a clear solution. Solubility in Formulation 2: ≥ 2.08 mg/mL (8.88 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one), clear solution. For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 20.8 mg/mL clear DMSO stock solution to 900 μL of corn oil and mix evenly. (Please use freshly prepared in vivo formulations for optimal results.) |
| 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.
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.
|
|
|
|
Products are for research use only; We do not sell to patients
Copyright 2020 InvivoChem LLC | All Rights Reserved
COA
