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.
| 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 | |
| Molecular Weight | 279.25 |
| Formula | C11H13N5O4 |
| CAS Number | 58131-57-0 |
| Solubility (25°C) | DMSO |
| Storage |
Powder -20°C 3 years ; 4°C 2 years In solvent -80°C 6 months ; -20°C 1 month |
| 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 Compound A used for a mouse (20 mg/kg) to a dose based on the BSA for a rat, multiply 20 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 Compound A of 10 mg/kg.
| Related Mdm2 Products |
|---|
| MMRi64
MMRi64 disrupts Mdm2-MdmX interactions. |
| MeOIstPyrd
MeOIstPyrd is an anti-skin cancer agent. |
| MDM2/XIAP-IN-3
MDM2/XIAP-IN-3 is a dual MDM2/XIAP inhibitor. |
| UNP-6457
UNP-6457 is a potent active MDM2-p53 interaction inhibitor with an IC50 values of 8.9 nM. |
| YL93
YL93 is a dual inhibitors of MDM2/4 with Ki values of 0.64 μM and 1.1 nM for MDM4 and MDM2, respectively. |
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