MI-773 (SAR405838)
Catalog No.S7649
Molecular Weight(MW): 562.50
MI-773 (SAR405838) is an orally available MDM2 antagonist with Ki of 0.88 nM. Phase 1.
Cited by 1 Publication
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A panel of four NB cell lines were seeded in six-well plates with indicated concentrations of SAR405838 and agar, and grown for 2 to 3 weeks. Cells were stained with crystal violet for 4 hours. Colonies were counted and colony numbers were represented as % vehicle ± S.D. with P < 0.05 (*), P < 0.01 (**) or P < 0.001 (***) (Student's t-test, two-tailed) as indicated.
Oncotarget, 2016, 7(50):82757-82769. MI-773 (SAR405838) purchased from Selleck.
Purity & Quality Control
Choose Selective Mdm2 Inhibitors
Biological Activity
| Description | MI-773 (SAR405838) is an orally available MDM2 antagonist with Ki of 0.88 nM. Phase 1. | ||||
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| In vitro |
MI-773 binds to MDM2 with Ki of 0.88 nM. MI-773 potently inhibits cell growth in cancer cell lines, including SJSA-1 (IC50, 0.092 μM), RS4;11 (IC50, 0.089 μM), LNCaP (IC50, 0.27 μM), and HCT-116 (IC50, 0.20 μM) cells, and displays high selectivity over cancer cell lines with mutated or deleted p53, including SAOS-2 (IC50, >10 μM), PC-3 (IC50, >10 μM), SW620 (IC50, >10 μM), and HCT-116 (p53-/-) (IC50, >20 μM) cells. [1] |
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| In vivo | In the SJSA-1 osteosarcoma, acute lymphoblastic leukemia RS4;11, LNCaP prostate cancer, and HCT-116 colon cancer xenograft model, MI-773 (p.o.) effectively inhibits tumor growth in a dose-dependent manner (10 mg/kg, 30 mg/kg, 50 mg/kg, 100 mg/kg, and 200 mg/kg,). [1] |
Protocol
| Kinase Assay:[1] |
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Fluorescence-polarization binding assay: Binding affinities of MDM2 inhibitors and p53 peptide to MDM2 protein are determined using an Fluorescence-polarization (FP) binding assay. Binding affinities of MI-773 to Bcl-2, Bcl-xL, Mcl-1, and β-catenin are determined using a competitive FP-based assay, and its binding affinity to MDMx is determined using Biolayer Interferometry technology. |
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| Cell Research:[1] |
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| Animal Research: [1] |
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Solubility (25°C)
| In vitro | DMSO | 100 mg/mL (177.77 mM) |
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| Ethanol | 31 mg/mL warmed (55.11 mM) | |
| Water | Insoluble |
* Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations.
Chemical Information
| Molecular Weight | 562.50 |
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| Formula | C29H34Cl2FN3O3 |
| CAS No. | 1303607-60-4 |
| Storage | powder |
| in solvent | |
| Synonyms | N/A |
Bio Calculators
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Clinical Trial Information
| NCT Number | Recruitment | Conditions | Sponsor/Collaborators | Start Date | Phases |
|---|---|---|---|---|---|
| NCT01985191 | Completed | Neoplasm Malignant | Sanofi|Merck KGaA | November 2013 | Phase 1 |
| NCT01636479 | Completed | Neoplasm Malignant | Sanofi | July 13 2012 | Phase 1 |
Tech Support
Answers to questions you may have can be found in the inhibitor handling instructions. Topics include how to prepare stock solutions, how to store inhibitors, and issues that need special attention for cell-based assays and animal experiments.
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