Size : 5mg
| Description | Nutlin-3a is the active enantiomer of Nutlin-3, an MDM2 antagonist that inhibits MDM2-p53 interaction (Ki=90 nM) and activates p53. Nutlin-3a binds preferentially to the p53-binding pocket of MDM2, leading to stabilization of p53 and activation of the p53 pathway. Nutlin-3a has antitumor activity. |
| Targets & IC50 | U-937 cells:15.6 μM, SKOV3 cells:38 μM, U2OS cells:3.35 μM, wild-type TP53 (HOC-7, OVCA429 and A2780 cells):4 - 6 μM, MDM2-p53 interaction:90 nM, OVAS cells:25 μM, Vero cells:> 50 μM, TOV21G cells:14 μM |
| In vitro | METHODS: N1E-115 cells were treated with Ionomycin calcium (0.2-10 µM) for 3-24 h. Cell viability was determined by trypan blue dye exclusion assay. RESULTS: Ionomycin calcium induced cell death in a concentration and time dependent manner. [1] METHODS: Fura-2-loaded mouse cerebellar astrocytes were treated with Ionomycin calcium (0.1-10 µM) for 35 min, and cell membrane Ca(2+) concentration was monitored by changes in the Fura-2 340/380 ratio. RESULTS: At concentrations ≤1 µM [Ca2+]c slowly declined after the initial peak, reaching significantly lower levels after 35 min. However, at 2 µM of ionomycin the peak level of [Ca2+]c was sustained in the plateau phase, and at concentrations >2 µM ionomycin [Ca2+]c was significantly higher after 35 min than at the initial peak. [2] |
| In vivo | METHODS: To investigate the mechanism of demyelination induced in vivo, Ionomycin calcium (2-50 µM, 0.5 µL) was dorsal column injected into SD rats. RESULTS: Rats injected with Ionomycin calcium showed varying degrees of lesions observed from days 1-21, including areas of localized edema, a small number of scattered demyelinated axons, and larger lesions containing up to 200 demyelinated or degenerated axons. [3] |
| Synonyms | Nutlin-3a chiral, (−)-Nutlin-3, (-)-Nutlin-3 |
| Kinase Assay | Biacore studies: Competition assays are performed on a Biacore S51. A Series S Sensor chip CM5 is derivatized for immobilization of a PentaHis antibody for capture of the His-tagged p53. The level of capture is ~ 200 response units (1 response unit corresponds to 1 pg of protein per mm 2). The concentration of MDM2 protein is kept constant at 300 nM. Test compounds are dissolved in DMSO at 10 mM and further diluted to make a concentration series of inhibitor in each MDM2 test sample. The assays are run at 25 °C in running buffer (10 mM Hepes, 0.15 M NaCl, 2% DMSO). MDM2-p53 binding in the presence of inhibitor is calculated as a percentage of binding in the absence of inhibitor and IC50 is calculated using Microsoft Excel |
| Cell Research | SRB(Only for Reference) |
| Molecular Weight | 581.49 |
| Formula | C30H30Cl2N4O4 |
| Cas No. | 675576-98-4 |
| Smiles | COc1ccc(C2=N[C@H]([C@H](N2C(=O)N2CCNC(=O)C2)c2ccc(Cl)cc2)c2ccc(Cl)cc2)c(OC(C)C)c1 |
| Relative Density. | 1.36 g/cm3 |
| Storage | Store at low temperature,Keep away from direct sunlight Powder: -20°C for 3 years | In solvent: -80°C for 1 year Shipping with blue ice/Shipping at ambient temperature. | ||||||||||||||||||||||||||||||||||||||||
| Solubility Information | Ethanol: 58.2 mg/mL (100.09 mM), Sonication is recommended. DMSO: 55 mg/mL (94.58 mM), Sonication is recommended.  | ||||||||||||||||||||||||||||||||||||||||
| In Vivo Formulation | 10% DMSO+40% PEG300+5% Tween 80+45% Saline: 2 mg/mL (3.44 mM), Sonication is recommended. Please add the solvents sequentially, clarifying the solution as much as possible before adding the next one. Dissolve by heating and/or sonication if necessary. Working solution is recommended to be prepared and used immediately. The formulation provided above is for reference purposes only. In vivo formulations may vary and should be modified based on specific experimental conditions. | ||||||||||||||||||||||||||||||||||||||||
Solution Preparation Table | |||||||||||||||||||||||||||||||||||||||||
DMSO/Ethanol
Ethanol
Note : The dilution table applies only to solid products. For liquid products, please calculate the stock solution based on the stated concentration and/or density. | |||||||||||||||||||||||||||||||||||||||||
For example, if the intended dosage is 10 mg/kg for animals weighing 20 g , with a dosing volume of 100 μL per animal, and a total of 10 animals are to be administered, using a formulation of 
10% DMSO+ 40% PEG300+ 5% Tween 80+ 45% Saline/PBS/ddH2O , the resulting working solution concentration would be 2 mg/mL.Dissolve 2 mg of the compound in 100 μL DMSO to obtain a stock solution at a concentration of 20 mg/mL . If the required concentration exceeds the compound's known solubility, please contact us for technical support before proceeding.
1) Add 100 μL of the DMSO stock solution to 400 µL PEG300 and mix thoroughly unt
