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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. 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,).
| Cell Experiment | |
|---|---|
| Cell lines | SJSA-1, RS4;11, LNCaP, SAOS-2, PC-3, SW620, HCT-116, and HCT-116 (p53-/-) cells |
| Preparation 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. |
| Concentrations | 100 μM |
| Incubation time | ~48 h |
| Animal Experiment | |
|---|---|
| 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. |
| Molecular Weight | 562.50 |
| Formula | C29H34Cl2FN3O3 |
| CAS Number | 1303607-07-9 |
| Solubility (25°C) | 100 mg/mL in DMSO |
| Storage |
Powder -20°C 3 years ; 4°C 2 years In solvent -80°C 6 months ; -20°C 1 month |
| Related Mdm2 Products |
|---|
| MMRi64
MMRi64 disrupts Mdm2-MdmX interactions. |
| MeOIstPyrd
MeOIstPyrd is an anti-skin cancer agent. |
| MDM2/XIAP-IN-3
MDM2/XIAP-IN-3 is a dual MDM2/XIAP inhibitor. |
| UNP-6457
UNP-6457 is a potent active MDM2-p53 interaction inhibitor with an IC50 values of 8.9 nM. |
| YL93
YL93 is a dual inhibitors of MDM2/4 with Ki values of 0.64 μM and 1.1 nM for MDM4 and MDM2, respectively. |
All AbMole products are for research use only, cannot be used for human consumption or veterinary use. We do not provide products or services to individuals. Please comply with the intended use and do not use AbMole products for any other purpose.
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