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SAR405838

SAR405838
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Purity:98.04%
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SAR405838

Catalog No. T6585Cas No. 1303607-60-4
MI-773 (SAR405838 (MI 773)) is an orally available MDM2 antagonist with Ki of 0.88 nM. Phase 1.
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Pack SizePriceAvailabilityQuantity
1 mg$45In Stock
2 mg$83In Stock
5 mg$135In Stock
10 mg$225In Stock
25 mg$441In Stock
50 mg$649In Stock
100 mg$926In Stock
500 mg$1,870In Stock
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Product Introduction

Bioactivity
Description
MI-773 (SAR405838 (MI 773)) is an orally available MDM2 antagonist with Ki of 0.88 nM. Phase 1.
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]
Kinase Assay
Fluorescence-polarization binding assay: Binding af?nities of MDM2 inhibitors and p53 peptide to MDM2 protein are determined using an Fluorescence-polarization (FP) binding assay. Binding af?nities of MI-773 to Bcl-2, Bcl-xL, Mcl-1, and β-catenin are determined using a competitive FP-based assay, and its binding af?nity to MDMx is determined using Biolayer Interferometry technology.
Cell Research
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)
AliasMI773, MI 773, MI-77301, MI-773
Chemical Properties
Molecular Weight562.5
FormulaC29H34Cl2FN3O3
Cas No.1303607-60-4
Storage & Solubility Information
StoragePowder: -20°C for 3 years | In solvent: -80°C for 1 year
Solubility Information
DMSO: 93 mg/mL (165.3 mM)
Ethanol: 29 mg/mL (51.6 mM)
H2O: < 1 mg/mL (insoluble or slightly soluble)
Solution Preparation Table
DMSO/Ethanol
1mg5mg10mg50mg
1 mM1.7778 mL8.8889 mL17.7778 mL88.8889 mL
5 mM0.3556 mL1.7778 mL3.5556 mL17.7778 mL
10 mM0.1778 mL0.8889 mL1.7778 mL8.8889 mL
20 mM0.0889 mL0.4444 mL0.8889 mL4.4444 mL
50 mM0.0356 mL0.1778 mL0.3556 mL1.7778 mL
DMSO
1mg5mg10mg50mg
100 mM0.0178 mL0.0889 mL0.1778 mL0.8889 mL

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