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Alrizomadlin
$320 – $5,400
Products Details
Product Description
– 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].
Web ID
– HY-101518
Storage Temperature
– -20°C, 3 years; 4°C, 2 years (Powder)
Shipping
– Room Temperature
Applications
– Cancer-programmed cell death
Molecular Formula
– C34H38Cl2FN3O4
References
– [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.
CAS Number
– 1818393-16-6
Molecular Weight
– 642.59
Compound Purity
– 98.67
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
Clinical Information
– Phase 2
Research Area
– Cancer
Solubility
– DMSO : 100 mg/mL (ultrasonic)
Target
– Apoptosis;E1/E2/E3 Enzyme;MDM-2/p53
Pathway
– Apoptosis;Metabolic Enzyme/Protease
Product type
– Reference compound
Disclaimer: All products are for research use only unless clearly stated otherwise on the product datasheet. Datasheets provided on the website are drafts for reference purpose only and you are requested to always refer to the hard copy included in the kit for your experimentation.
