Appearance:Solid powderPurity: > 98%
AA-115, also known as APG-115, is a highly potent, chemically stable and efficacious MDM2 inhibitor, which has entered clinical development for cancer treatment. AA-115 has a very high affinity to MDM2 (Ki < 1 nM), potent cellular activity, and an excellent oral pharmacokinetic profile. Compound 60 is capable of achieving complete and longlasting tumor regression in vivo and is currently in phase I clinical trials for cancer treatment.
1:J Med Chem. 2017 Apr 13;60(7):2819-2839. doi: 10.1021/acs.jmedchem.6b01665. Epub 2017 Mar 24. Discovery of 4-((3/'R,4/'S,5/'R)-6″-Chloro-4/'-(3-chloro-2-fluorophenyl)-1/'-ethyl-2″-oxodispiro[cyclohexane-1,2/'-pyrrolidine-3/',3″-indoline]-5/'-carboxamido)bicyclo[2.2.2]octane-1-carboxylic Acid (AA-115/APG-115): A Potent and Orally Active Murine Double Minute 2 (MDM2) Inhibitor in Clinical Development.Aguilar A,Lu J,Liu L,Du D,Bernard D,McEachern D,Przybranowski S,Li X,Luo R,Wen B,Sun D,Wang H,Wen J,Wang G,Zhai Y,Guo M,Yang D,Wang S, PMID: 28339198 PMCID: PMC5394527 DOI: 10.1021/acs.jmedchem.6b01665 Abstract: We previously reported the design of spirooxindoles with two identical substituents at the carbon-2 of the pyrrolidine core as potent MDM2 inhibitors. In this paper we describe an extensive structure-activity relationship study of this class of MDM2 inhibitors, which led to the discovery of 60 (AA-115/APG-115). Compound 60 has a very high affinity to MDM2 (Ki < 1 nM), potent cellular activity, and an excellent oral pharmacokinetic profile. Compound 60 is capable of achieving complete and long-lasting tumor regression in vivo and is currently in phase I clinical trials for cancer treatment.