MI-773 |
Catalog No.GC16296 |
MI-773 es un potente inhibidor de la interacciÓn proteÍna-proteÍna (PPI) de MDM2-p53 con alta afinidad de uniÓn contra MDM2 (Kd=8,2 nM). MI-773 tiene actividad antitumoral.
Products are for research use only. Not for human use. We do not sell to patients.
Cas No.: 1303607-07-9
Sample solution is provided at 25 µL, 10mM.
MI-773 is a small molecule inhibitor of MDM2 with IC50 value of 62nM [1].
MI-773 is a small molecule MDM2 antagonist. It is a spirooxindole derivative. MI-773 shows a high MDM2 affinity with IC50 value of 62nM in the FP competitive binding experiment. In the in vitro cell-based assay, MI-773 shows a similar inhibition efficacy with its enantiomer MI-77301. The GI50 values are 58nM and 33nM for MI-773 and MI-77301, respectively. Both MI-773 and MI-77301 exert considerable activity at dose of 100 mg/kg in mouse xenograft models of osteosarcoma, prostate cancer, colorectal cancer, leukemia or melanoma. Currently, an international and multicenter phase I trial of MI-773 is underway for patients with liposarcomas and other p53-wild-type tumors [1, 2].
References:
[1] Zak K, Pecak A, Rys B, Wladyka B, Dömling A, Weber L, Holak TA, Dubin G. Mdm2 and MdmX inhibitors for the treatment of cancer: a patent review (2011-present). Expert Opin Ther Pat. 2013 Apr;23(4):425-48.
[2] Shoushtari AN, Van Tine BA, Schwartz GK. Novel treatment targets in sarcoma: more than just the GIST. Am Soc Clin Oncol Educ Book. 2014:e488-95.
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