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Alrizomadlin

Catalog No. T14303   CAS 1818393-16-6
Synonyms: APG-115, AA-115

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

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Alrizomadlin Chemical Structure
Alrizomadlin, CAS 1818393-16-6
Pack Size Availability Price/USD Quantity
1 mg In stock $ 263.00
2 mg In stock $ 377.00
5 mg In stock $ 622.00
10 mg In stock $ 888.00
25 mg In stock $ 1,330.00
50 mg In stock $ 1,790.00
100 mg In stock $ 2,430.00
500 mg In stock $ 4,880.00
1 mL * 10 mM (in DMSO) In stock $ 786.00
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Purity: 98.79%
Purity: 98.69%
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Biological Description
Chemical Properties
Storage & Solubility Information
Description Alrizomadlin (APG-115) is an orally active inhibitor of MDM2 with IC50 of 3.8 nM and Ki of 1 nM, respectively[1]. Alrizomadlin blocks the interaction of MDM2 and p53 and induces cell-cycle arrest and apoptosis in a p53-dependent manner.
Targets&IC50 MDM2:3.8 nM
In vitro Alrizomadlin (0.001-100 μM) inhibits cell proliferation in a concentration-dependent manner(IC50s: 18.9 nM and 103.5 ± 18.3 nM respectively in AGS and MKN45 cells). Alrizomadlin (0.02-0.2 μM) activates p53 to enhance radiosensitivity in AGS and MKN45 cells and enhances the anti-proliferative effect of radiotherapy at different radiation doses. Stable knockout of p53 abrogates expression of MDM2, p53, p21, PUMA, BAX, Cleaved-caspase3, γH2AX. Alrizomadlin affects progression by inducing cells arrested at G0/G1 phase[3]. Alrizomadlin (0.3 μM-10 μM) leads to a concentration-dependent cell cycle arrest in G2/M phases and decreases S-phase in p53 wide-type cell lines (TPC-1, KTC-1)[4].
In vivo In male BALB/c athymic nude mice with MKN45 cells, Alrizomadlin (100 mg/kg; orally) enhances radiation antitumor effect in gastric adenocarcinoma[3].
Synonyms APG-115, AA-115
Molecular Weight 642.59
Formula C34H38Cl2FN3O4
CAS No. 1818393-16-6

Storage

Powder: -20°C for 3 years | In solvent: -80°C for 1 year

Solubility Information

DMSO: 90 mg/mL (140.1 mM), Sonification is recommended.

TargetMolReferences and Literature

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 pembrolizumab 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.

Related compound libraries

This product is contained In the following compound libraries:
Anti-Cancer Drug Library Drug Repurposing Compound Library Inhibitor Library Anti-Cancer Clinical Compound Library Anti-Cancer Active Compound Library Clinical Compound Library Bioactive Compound Library Bioactive Compounds Library Max Anti-Cancer Compound Library PPI Inhibitor Library

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Kevetrin hydrochloride p53-Mdm2 inhibitor 4 Triptolide MI-1061 Ganoderic acid X MX69 p53-MDM2-IN-1 MG-277

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Keywords

Alrizomadlin 1818393-16-6 Apoptosis Mdm2 AA 115 APG-115 APG115 AA115 APG 115 AA-115 inhibitor inhibit

 

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