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25mg |
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Purity: ≥98%
NSC 207895 is a novel anticancer agent that is able to suppress MDM2 with an IC50 of 2.5 μM, which leads to enhanced p53 stabilization/activation and DNA damage. Therefore, it is a p53 activator that also controls MDM2, an E3 ligase. NSC 207895 is a less toxic benzofuroxan derivative. NSC 207895 lowers the activity of the MDMX promoter, which in turn lowers the mRNA and protein levels of MDMX in MCF-7 cells. The activation of p53 coincides with this inhibition of MDMX.
Targets |
MDMX (IC50 = 2.5 μM)
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ln Vitro |
In MCF-7 cells, NSC-207895 reduces MDMX protein and mRNA levels. In MCF-7 cells, NSC-207895 inducibly upregulates the expression of p53 as well as the well-known p53-target genes, p21 and MDM2, in a dose-dependent manner. Cycloheximide chase assays in MCF-7 cells showed that NSC-207895 prolongs the half-life of p53 from 20 to 30 minutes to more than 3 hours. Additionally, NSC-207895 stimulates the expression of p21, MDM2, and p53 in LNCaP prostate cancer cells and A549 lung cancer cells. In MCF-7 cells, NSC-207895 increases the mRNA levels of proapoptotic genes such as PUMA, BAX, and PIG3 in a dose-dependent manner. Sub-G0/G1 cell counts and G2 arrest both significantly rise in response to NSC-207895. Additionally, NSC-207895 lowers cell viability in A549 and LNCaP cells and causes more than 40% of cells to die through apoptosis. [1] In L1210 cells, NSC-207895 prevents the biosynthesis of nucleic acids and proteins. [2] NSC-207895 interacts with DNA repair to activate the DNA damage repair pathway in three species (S. cerevisiae, S. pombe, and H. sapiens).[3] NSC-207895 has a GI50 of 117 nM and is cytotoxic to the G/R-luc astrocytoma cell line.[4]
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ln Vivo |
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Cell Assay |
Dimethyl sulfoxide (DMSO), nutlin-3a, or NSC-207895-treated MCF-7 cells are permeabilized with cold 70% ethanol overnight, and then stained with a solution containing 50 g/mL propidium iodide and 20 g/mL RNase A at 37 °C for 20 minutes. After that, the cells are analyzed using flow cytometry. Calculating the proportion of cells in each cell cycle phase uses the FlowJo program. For terminal deoxynucleotidyl transferase-mediated dUTP nick end labeling (TUNEL) staining, NSC-207895-treated MCF-7 cells are fixed with 4% paraformaldehyde for 1 hour, followed by dUTP labeling using In Situ Cell Death Detection Kit TMR Red in accordance with the manufacturer's instructions. At least 300 cells are randomly selected for quantitation, and the number of TUNEL-positive cells is counted.
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Animal Protocol |
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References |
Molecular Formula |
C11H13N5O4
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Molecular Weight |
279.25
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Exact Mass |
279.10
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Elemental Analysis |
C, 47.31; H, 4.69; N, 25.08; O, 22.92
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CAS # |
58131-57-0
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Related CAS # |
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Appearance |
Solid powder
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SMILES |
CN1CCN(CC1)C2=CC=C(C3=NO[N+](=C23)[O-])[N+](=O)[O-]
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InChi Key |
MWFZDJLPWDCQIL-UHFFFAOYSA-N
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InChi Code |
InChI=1S/C11H13N5O4/c1-13-4-6-14(7-5-13)9-3-2-8(15(17)18)10-11(9)16(19)20-12-10/h2-3H,4-7H2,1H3
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Chemical Name |
4-(4-methylpiperazin-1-yl)-7-nitro-3-oxido-2,1,3-benzoxadiazol-3-ium
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Synonyms |
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HS Tariff Code |
2934.99.9001
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Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month Note: This product requires protection from light (avoid light exposure) during transportation and storage. |
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Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
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Solubility (In Vitro) |
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Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.08 mg/mL (7.45 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 (7.45 mM) in 10% DMSO + 90% (20% SBE-β-CD in Saline) (add these co-solvents sequentially from left to right, and one by one), suspension solution; with ultrasonication. 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 20% SBE-β-CD physiological saline solution and mix evenly. Preparation of 20% SBE-β-CD in Saline (4°C,1 week): Dissolve 2 g SBE-β-CD in 10 mL saline to obtain a clear solution.  (Please use freshly prepared in vivo formulations for optimal results.) |
Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
1 mM | 3.5810 mL | 17.9051 mL | 35.8102 mL | |
5 mM | 0.7162 mL | 3.5810 mL | 7.1620 mL | |
10 mM | 0.3581 mL | 1.7905 mL | 3.5810 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.