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AA-115 CAS: 1818393-16-6

Category: Inhibitors
Product Name: AA-115
Cat No: I000330
CAS No: 1818393-16-6
Synonyms: AA-115; AA 115; AA115; APG 115; APG115; APG-115.;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
Molecular Formula: C34H38Cl2FN3O4
Molecular Weight: 642.5934
SMILES: O=C1NC2=CC(Cl)=CC=C2[C@]13C4(CCCCC4)N(CC)[C@@H](C(NC5(CC6)CCC6(C(O)=O)CC5)=O)[C@@H]3C7=C(F)C(Cl)=CC=C7
InChI: InChI=1S/C34H38Cl2FN3O4/c1-2-40-27(28(41)39-32-16-13-31(14-17-32,15-18-32)30(43)44)25(21-7-6-8-23(36)26(21)37)34(33(40)11-4-3-5-12-33)22-10-9-20(35)19-24(22)38-29(34)42/h6-10,19,25,27H,2-5,11-18H2,1H3,(H,38,42)(H,39,41)(H,43,44)/t25-,27+,31?,32?,34+/m0/s1
InChIKey: YJCZPJQGFSSFOL-MNZPCBJKSA-N
Solubility: Soluble in DMSO
Target: MDM2 inhibitor
CAS 1818393-16-6,AA-115
  • Description

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.

  • Spec

Appearance:Solid powder
Purity: > 98%

  • References

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.


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