MI-773 (SAR405838)

Catalog No.S7649

MI-773 (SAR405838) Chemical Structure

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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1 Customer Review

  • 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.

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Biological Activity

Description MI-773 (SAR405838) is an orally available MDM2 antagonist with Ki of 0.88 nM. Phase 1.
Targets
p53 [1] MDM2 [1]
(Cell-free assay)
0.88 nM(Ki)
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]

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.
Cell Research:[1]
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  • Cell lines: SJSA-1, RS4;11, LNCaP, SAOS-2, PC-3, SW620, HCT-116, and HCT-116 (p53-/-) cells
  • Concentrations: 100 μM
  • Incubation Time: ~48 h
  • Method: Cell growth inhibition activity is determined in a water-soluble tetrazolium-based assay. Cell death is measured by trypan blue staining and apoptosis is determined using an Annexin V-FLUOS staining kit.
    (Only for Reference)
Animal Research: [1]
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  • Animal Models: SCID mice with SJSA-1 osteosarcoma (females), acute lymphoblastic leukemia RS4;11 (females), LNCaP prostate cancer (males), or HCT-116 colon cancer (females) xenograft model
  • Formulation: 10% PEG400: 3% Cremophor: 87% PBS, or 2% TPGS: 98% PEG200
  • Dosages: 200 mg/kg
  • Administration: p.o.
    (Only for Reference)

Solubility (25°C)

In vitro DMSO 100 mg/mL (177.77 mM)
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
Formula

C29H34Cl2FN3O3

CAS No. 1303607-60-4
Storage powder
Synonyms N/A

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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 Active, not recruiting Neoplasm Malignant Sanofi July 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.

Handling Instructions

Tel: +1-832-582-8158 Ext:3

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Mdm2 Signaling Pathway Map

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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID