Powder: -20°C for 3 years
In solvent: -80°C for 2 years
MI-773 (SAR405838) is an orally available MDM2 antagonist with Ki of 0.88 nM. Phase 1.
Description | MI-773 (SAR405838) is an orally available MDM2 antagonist with Ki of 0.88 nM. Phase 1. |
Targets&IC50 | MDM2:0.88 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] |
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) |
Synonyms | MI773, MI-77301, MI 773, MI-773 |
Molecular Weight | 562.51 |
Formula | C29H34Cl2FN3O3 |
CAS No. | 1303607-60-4 |
Powder: -20°C for 3 years
In solvent: -80°C for 2 years
DMSO: 93 mg/mL (165.3 mM)
Ethanol: 29 mg/mL (51.6 mM)
H2O: <1 mg/mL
( < 1 mg/ml refers to the product slightly soluble or insoluble )
You can also refer to dose conversion for different animals. More
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Please see Inhibitor Handling Instructions for more frequently ask questions. Topics include: how to prepare stock solutions, how to store products, and cautions on cell-based assays & animal experiments, etc.
SAR405838 1303607-60-4 凋亡 泛素化 E1/E2/E3 Enzyme Mdm2 MDM-2/p53 MI773 SAR-405838 Ubiquitin activating enzyme inhibit Ubiquitin ligase Inhibitor MI 77301 SAR 405838 Ubiquitin conjugating enzyme E2 conjugating enzyme E3 ligating enzyme E1 activating enzyme MI-77301 MI 773 MI-773 MI77301 inhibitor