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Idasanutlin (Ro 5503781) (RG-7388) is an effective and specific p53-MDM2 inhibitor (IC50: 6 nM).
Pack Size | Price | Availability | Quantity |
---|---|---|---|
2 mg | $34 | In Stock | |
5 mg | $55 | In Stock | |
10 mg | $97 | In Stock | |
25 mg | $162 | In Stock | |
50 mg | $238 | In Stock | |
100 mg | $396 | In Stock | |
500 mg | $929 | In Stock | |
1 mL x 10 mM (in DMSO) | $76 | In Stock |
Description | Idasanutlin (Ro 5503781) (RG-7388) is an effective and specific p53-MDM2 inhibitor (IC50: 6 nM). |
Targets&IC50 | MDM2:6 nM |
In vitro | Idasanutlin inhibits cell proliferation with IC50 of 30 nM, and induces dose-dependent p53 stabilization, cell cycle arrest, as well as cell apoptosis in cancer cells expressing wild-type p53. [1] |
In vivo | In a mouse SJSA human osteosarcoma xenograft model, Idasanutlin (25 mg/kg p.o.) causes tumor growth inhibition and regression. [1] In a SJSA xenograft model, Idasanutlin results in induction of apoptosis and antiproliferation. [2] |
Kinase Assay | Biochemical Binding Affinity – HTRF Assay: The p53-MDM2 HTRF assay is performed in buffer containing 50 mM Tris-HCl, pH 7.4, 100 mM NaCl, 1 mM DTT, 0.02 or 0.2 mg/ml BSA. Small-molecule inhibitors are stored in aliquots as 10 mM stock solutions in DMSO at 4°C in 96-deep-well plates. It is thawed and mixed immediately prior to testing. The compound is incubated with GST-MDM2 and a biotinylated p53 peptide for one hour at 37°C. Phycolink goat anti-GST (Type 1) allophycocyanin and Eu-8044-streptavidin are then added and followed by one hour incubation at room temperature. Plates are read using the Envision fluorescence reader. IC50 values are determined from inter-plate duplicate or triplicate sets of data. Data are analyzed by XLfit4 (Microsoft) using a 4 Parameter Logistic Model (Sigmoidal Dose-Response Model) and the equation Y= (A+ ((B-A)/ (1+ ((C/x)^D)))), where A and B are enzyme activity in the absence or presence of infinite inhibitor compound, respectively, C is the IC50 and D is the Hill coefficient. |
Cell Research | Cell proliferation is evaluated by the tetrazolium dye assay. The concentration at which 50% inhibition (IC50) or 90% inhibition (IC90) of cell proliferation is determined from the linear regression of a plot of the logarithm of the concentration versus percent inhibition. (Only for Reference) |
Alias | Ro 5503781, RG7388 |
Molecular Weight | 616.48 |
Formula | C31H29Cl2F2N3O4 |
Cas No. | 1229705-06-9 |
Smiles | COc1cc(ccc1NC(=O)C1NC(CC(C)(C)C)C(C#N)(C1c1cccc(Cl)c1F)c1ccc(Cl)cc1F)C(O)=O |
Relative Density. | 1.40 g/cm3 (Predicted) |
Storage | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice. | |||||||||||||||||||||||||||||||||||
Solubility Information | H2O: < 1 mg/mL (insoluble or slightly soluble) DMSO: 55 mg/mL (89.22 mM) Ethanol: 8 mg/mL (12.97 mM), Heating is recommended. | |||||||||||||||||||||||||||||||||||
Solution Preparation Table | ||||||||||||||||||||||||||||||||||||
Ethanol/DMSO
DMSO
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