Alrizomadlin

Alrizomadlin (APG-115) is an orally active MDM2 protein inhibitor binding to MDM2 protein with IC50 and Ki values of 3.8 nM and 1 nM, respectively[1]. Alrizomadlin blocks the interaction of MDM2 and p53 and induces cell-cycle arrest and apoptosis in a p53-dependent manner[2][3].

Product Specifications

CAS Number

[1818393-16-6]

Product Name Alternative

APG-115; AA-115

UNSPSC

12352005

Target

Apoptosis; E1/E2/E3 Enzyme; MDM-2/p53

Type

Reference compound

Related Pathways

Apoptosis; Metabolic Enzyme/Protease

Applications

Cancer-programmed cell death

Field of Research

Cancer

Assay Protocol

https://www.medchemexpress.com/apg-115.html

Concentration

10mM

Purity

98.57

Solubility

DMSO : 100 mg/mL (ultrasonic)

Smiles

O=C(N1)[C@]([C@@H](C(C=CC=C2Cl)=C2F)[C@@H]3C(NC45CCC(C(O)=O)(CC5)CC4)=O)(C(C1=C6)=CC=C6Cl)C7(CCCCC7)N3CC

Molecular Formula

C34H38Cl2FN3O4

Molecular Weight

642.59

References & Citations

[1]Angelo Aguilar, et al. 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. J Med Chem. 2017 Apr 13; 60 (7) : 2819–2839.|[2]A W Tolcher et al, A phase Ib/II study of APG-115 in combination with MK-3475 in patients with unresectable or metastatic melanomas or advanced solid tumors, Ann Oncol. 2019 Feb 1; 30 (Supplement_1) . pii: mdz027.|[3]Hanjie Yi ea al, A novel small molecule inhibitor of MDM2-p53 (APG-115) enhances radiosensitivity of gastric adenocarcinoma, J Exp Clin Cancer Res. 2018 May 2;37 (1) :97.|[4]Chen H, et al. Restoration of p53 using the novel MDM2-p53 antagonist APG115 suppresses dedifferentiated papillary thyroid cancer cells. Oncotarget. 2017 Jun 27;8 (26) :43008-43022.