NSC 207895

Alias: NSC-207895; NSC207895; XI-006; XI006; XI 006; NSC 207895; NSC-179940; NSC179940; NSC 179940
Cat No.:V0041 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.
NSC 207895 Chemical Structure CAS No.: 58131-57-0
Product category: Mdm2
This product is for research use only, not for human use. We do not sell to patients.
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Purity & Quality Control Documentation

Purity: ≥98%

Product Description

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.

Biological Activity I Assay Protocols (From Reference)
Targets
MDMX (IC50 = 2.5 μM)
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]
ln Vivo

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.
Animal Protocol


References

[1]. Mol Cancer Ther . 2011 Jan;10(1):69-79.

[2]. Cancer Res . 1975 Dec;35(12):3735-40.

[3]. Mol Syst Biol . 2010 Dec 21:6:451.

[4]. J Biomol Screen . 2008 Sep;13(8):795-803.

These protocols are for reference only. InvivoChem does not independently validate these methods.
Physicochemical Properties
Molecular Formula
C11H13N5O4
Molecular Weight
279.25
Exact Mass
279.10
Elemental Analysis
C, 47.31; H, 4.69; N, 25.08; O, 22.92
CAS #
58131-57-0
Appearance
Solid powder
SMILES
CN1CCN(CC1)C2=CC=C(C3=NO[N+](=C23)[O-])[N+](=O)[O-]
InChi Key
MWFZDJLPWDCQIL-UHFFFAOYSA-N
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
Chemical Name
4-(4-methylpiperazin-1-yl)-7-nitro-3-oxido-2,1,3-benzoxadiazol-3-ium
Synonyms
NSC-207895; NSC207895; XI-006; XI006; XI 006; NSC 207895; NSC-179940; NSC179940; NSC 179940
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: ~0.4 mg/mL (~1.43 mM)
Water: <1 mg/mL (slightly soluble or insoluble)
Ethanol: <1 mg/mL
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.

Calculator

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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)
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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.
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Biological Data
  • NSC 207895

    NSC-207895 is a DNA damaging agent. Molecular Systems Biology 6(1):451 December 2010 
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