| 名称 | SAR405838 |
| 描述 | MI-773 (SAR405838 (MI 773)) is an orally available MDM2 antagonist with Ki of 0.88 nM. Phase 1. |
| 细胞实验 | 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) |
| 激酶实验 | 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. |
| 体外活性 | SAR405838 binds to MDM2 with Ki of 0.88 nM. SAR405838 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] |
| 体内活性 | In the SJSA-1 osteosarcoma, acute lymphoblastic leukemia RS4;11, LNCaP prostate cancer, and HCT-116 colon cancer xenograft model, SAR405838 (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] |
| 存储条件 | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice. |
| 溶解度 | DMSO : 93 mg/mL (165.3 mM)
Ethanol : 29 mg/mL (51.6 mM)
H2O : < 1 mg/mL (insoluble or slightly soluble)
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| 关键字 | MDM-2/p53 | SAR 405838 | Ubiquitin activating enzyme | MI77301 | inhibit | Ubiquitin ligase | Inhibitor | MI 77301 | Ubiquitin conjugating enzyme | E2 conjugating enzyme | SAR-405838 | E3 ligating enzyme | SAR405838 | E1 activating enzyme | E1/E2/E3 Enzyme |
| 相关产品 | Milademetan | NSC697923 | XI-006 | PYZD-4409 | Nutlin-3 | NAcM-OPT | PYR-41 | NSC232003 | NAE-IN-M22 | Indole-3-carbinol | Idasanutlin | RITA |
United States
