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.
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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 | interventions | Conditions | Sponsor/Collaborators | Start Date | Phases |
|---|---|---|---|---|---|---|
| NCT01985191 | Completed | Drug: SAR405838|Drug: Pimasertib | Neoplasm Malignant | Sanofi|Merck KGaA Darmstadt Germany | November 2013 | Phase 1 |
| NCT01636479 | Completed | Drug: SAR405838 | Neoplasm Malignant | Sanofi | July 13 2012 | Phase 1 |
Tech Support
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