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NSC 207895

Cat. No. M3224

NSC 207895 Structure

Synonym: XI-006

Size Price Availability Quantity
5mg USD 140 In stock
10mg USD 260 In stock
50mg USD 780 In stock
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Quality Control
  • Current batch:
  • Purity >99%
  • COA
  • MSDS
Biological Activity

NSC-207895 (XI-006) is a derivative of nitrobenzofuroxan and an anticancer agent with an EC50 of 1 μM. NSC-207895 (XI-006) is a highly electrophilic compound known to have both antitumor and mutagenic activities. NSC-207895 (XI-006) may lead to the damage of DNA that inhibits the growth of tumors. NSC-207895 (XI-006) strikingly prevented the expression of MDMX which is a p53-binding protein and modulate the activities and stabilities of p53. NSC-207895 (XI-006) is less toxic and reduced the activities of MDMX promoter in a dose-dependent manner. Moreover,NSC-207895 (XI-006)  possibly decreased the expression of MDMX via suppressing MDMX transcription. However, NSC-207895 (XI-006) induced the expression of MDM2 which is also a p53 downstream gene, despite to a less extent. In addition, NSC-207895 (XI-006) also upregulated the expression of p53 in MCF-7 cells that led to increased expression of proapoptotic genes including PUMA, BAX, as well as PIG3. Notably, NSC-207895 (XI-006), also called a small-molecule p53 activator, gives rise to MCF-7 cells to experience apoptosis and decrease the viability of cancer cells along with nutlin-3a, which dissociated the MDM2-p53 complex.

Protocol
Cell Experiment
Cell lines MCF-7 cell
Preparation method Treating MCF-7 cells with dimethyl sulfoxide (DMSO), nutlin-3a, or NSC-207895 are permeabilized with cold 70% ethanol overnight, and staining with a solution containing 50 μg/mL propidium iodide and 20 μg/mL RNase A at 37°C for 20 minutes. And then subjected the cells to flow cytometry analysis. Using the FlowJo software to calculate percentages of cells in each cell cycle phase. For terminal deoxynucleotidyl transferase–mediated dUTP nick end labeling (TUNEL) staining,according to the manufacturer's protocol, MCF-7 cells treated with the NSC-207895 for 2 days are fixed with 4% paraformadelhyde for 1 hour, and then subjected to dUTP labeling using In Situ Cell Death Detection Kit TMR Red . For quantitation, choose at least 300 cells randomly and count the numbers of TUNEL-positive cells .
Concentrations 1-10 μM
Incubation time 2 days
Animal Experiment
Animal models
Formulation
Dosages
Administration
Conversion of different model animals based on BSA (Value based on data from FDA Draft Guidelines)
Species Mouse Rat Rabbit Guinea pig Hamster Dog
Weight (kg) 0.02 0.15 1.8 0.4 0.08 10
Body Surface Area (m2) 0.007 0.025 0.15 0.05 0.02 0.5
Km factor 3 6 12 8 5 20
Animal A (mg/kg) = Animal B (mg/kg) multiplied by  Animal B Km
Animal A Km

For example, to modify the dose of resveratrol used for a mouse (22.4 mg/kg) to a dose based on the BSA for a rat, multiply 22.4 mg/kg by the Km factor for a mouse and then divide by the Km factor for a rat. This calculation results in a rat equivalent dose for resveratrol of 11.2 mg/kg.

Chemical Information
Molecular Weight 279.25
Formula C11H13N5O4
CAS Number 58131-57-0
Purity >99%
Solubility DMSO
Storage at -20°C
Related Mdm2 Products
MI-773

MI-773 is an orally available MDM2 antagonist with Ki of 0.88 nM.

Kevetrin hydrochloride

Kevetrin hydrochloride is a small molecule and activator of the tumor suppressor protein p53, with potential antineoplastic activity.

RG7112

RG7112 is the first clinical small-molecule MDM2 inhibitor designed to occupy the p53-binding pocket of MDM2.

SL-01

SL-01 is a p53-Mdm2 interaction inhibitor with IC50 of 3.18 μM.

Nutlin-3b

Nutlin-3b is a p53/MDM2 antagonist or inhibitor with IC50 value of 13.6 μM, 150-fold less potent (+)-enantiomer of Nutlin-3 as in comparison with opposite enantiomer Nutlin-3a.

  Catalog
Abmole Inhibitor Catalog 2017




Keywords: NSC 207895, XI-006 supplier, Mdm2, inhibitors

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