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MI-773

Cat. No. M5225

MI-773 Structure
Size Price Availability Quantity
5mg USD 178 In stock
10mg USD 295 In stock
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Quality Control
  • Current batch:
  • Purity >99%
  • COA
  • MSDS
Biological Activity

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,).

Protocol
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.
Conversion of different model animals based on BSA (Value based on data from FDA Draft Guidelines)
Species Mouse Rat Rabbit Guinea pig Hamster Dog
Weight (kg) 0.02 0.15 1.8 0.4 0.08 10
Body Surface Area (m2) 0.007 0.025 0.15 0.05 0.02 0.5
Km factor 3 6 12 8 5 20
Animal A (mg/kg) = Animal B (mg/kg) multiplied by  Animal B Km
Animal A Km

For example, to modify the dose of resveratrol used for a mouse (22.4 mg/kg) to a dose based on the BSA for a rat, multiply 22.4 mg/kg by the Km factor for a mouse and then divide by the Km factor for a rat. This calculation results in a rat equivalent dose for resveratrol of 11.2 mg/kg.

Chemical Information
Molecular Weight 562.50
Formula C29H34Cl2FN3O3
CAS Number 1303607-07-9
Purity >99%
Solubility 100 mg/mL in DMSO
Storage at -20°C
References

Novel MDM2 inhibitor SAR405838 (MI-773) induces p53-mediated apoptosis in neuroblastoma.
Lu J, et al. Oncotarget. 2016 Dec 13;7(50):82757-82769. PMID: 27764791.

Therapeutic Inhibition of the MDM2-p53 Interaction Prevents Recurrence of Adenoid Cystic Carcinomas.
Nör F, et al. Clin Cancer Res. 2017 Feb 15;23(4):1036-1048. PMID: 27550999.

SAR405838: an optimized inhibitor of MDM2-p53 interaction that induces complete and durable tumor regression.
Wang S, et al. Cancer Res. 2014 Oct 15;74(20):5855-65. PMID: 25145672.

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  Catalog
Abmole Inhibitor Catalog 2017




Keywords: MI-773 supplier, Mdm2, inhibitors

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