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Alrizomadlin

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Purity:98.79%

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COA HNMR HPLC

Alrizomadlin

Catalog No. T14303Cas No. 1818393-16-6

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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Pack Size	Price	Availability
1 mg	$263	In Stock
5 mg	$619	In Stock
10 mg	$888	In Stock
25 mg	$1,270	In Stock
50 mg	$1,530	In Stock
100 mg	$1,990	In Stock
1 mL x 10 mM (in DMSO)	$786	In Stock

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Product Introduction

Bioactivity

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.
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].
Alias	APG-115, AA-115

Chemical Properties

Molecular Weight	642.59
Formula	C34H38Cl2FN3O4
Cas No.	1818393-16-6

Storage & Solubility Information

Storage

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

Solubility Information

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

Solution Preparation Table

DMSO

	1mg	5mg	10mg	50mg
1 mM	1.5562 mL	7.7810 mL	15.5620 mL	77.8101 mL
5 mM	0.3112 mL	1.5562 mL	3.1124 mL	15.5620 mL
10 mM	0.1556 mL	0.7781 mL	1.5562 mL	7.7810 mL
20 mM	0.0778 mL	0.3891 mL	0.7781 mL	3.8905 mL
50 mM	0.0311 mL	0.1556 mL	0.3112 mL	1.5562 mL
100 mM	0.0156 mL	0.0778 mL	0.1556 mL	0.7781 mL

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Mother liquor preparation method: 2 mg of drug dissolved in 50 μL DMSO TargetMol | reagent

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Preparation method for in vivo formula: Take 50 μL DMSO TargetMol | reagent

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