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Alrizomadlin
Alrizomadlin (APG-115) is an orally active MDM2 inhibitor with an IC50 of 3.8 nM and a Ki of 1 nM[1]. It blocks the interaction of MDM2 and p53, inducing cell-cycle arrest and apoptosis in a p53-dependent manner.
Catalog No. T14303Cas No. 1818393-16-6
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Purity:98.79%
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Alrizomadlin
Catalog No. T14303Cas No. 1818393-16-6
Alrizomadlin (APG-115) is an orally active MDM2 inhibitor with an IC50 of 3.8 nM and a Ki of 1 nM[1]. It blocks the interaction of MDM2 and p53, inducing cell-cycle arrest and apoptosis in a p53-dependent manner.
All TargetMol products are for research purposes only and cannot be used for human consumption. We do not provide products or services to individuals. Please comply with the intended use and do not use TargetMol products for any other purpose. | Pack Size | Price | Availability | Quantity |
|---|---|---|---|
| 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
Chemical Properties
Storage & Solubility Information
| Description | Alrizomadlin (APG-115) is an orally active MDM2 inhibitor with an IC50 of 3.8 nM and a Ki of 1 nM[1]. It blocks the interaction of MDM2 and p53, inducing 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]. |
| Alias | 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 | Shipping with blue ice. | |||||||||||||||||||||||||||||||||||
| Solubility Information | DMSO: 90 mg/mL (140.1 mM), Sonication is recommended. | |||||||||||||||||||||||||||||||||||
Solution Preparation Table | ||||||||||||||||||||||||||||||||||||
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In Vivo Formulation Calculator (Clear solution)
Please enter your animal experiment information in the following box and click Calculate to obtain the mother liquor preparation method and in vivo formula preparation method:
For example, your dosage is 10 mg/kg Each animal weighs 20 g, and the dosage volume is 100 μL . A total of 10 animals were administered, and the formula you used is 5% 
DMSO+30% PEG300+5% Tween 80+60% ddH2O. So your working solution concentration is 2 mg/mL。Mother liquor preparation method: 2 mg of drug dissolved in 50 μL DMSO (mother liquor concentration of 40 mg/mL), if you need to configure a concentration that exceeds the solubility of the product, please contact us first.
(mother liquor concentration of 40 mg/mL), if you need to configure a concentration that exceeds the solubility of the product, please contact us first.Preparation method for in vivo formula: Take 50 μL DMSO main solution, add 300 μLPEG300 mix well and clarify, then add 50 more μL Tween 80, mix well and clarify, then add 600 more μLddH2O mix well and clarify
main solution, add 300 μLPEG300 mix well and clarify, then add 50 more μL Tween 80, mix well and clarify, then add 600 more μLddH2O mix well and clarifyFor Reference Only. Please develop an appropriate dissolution method based on your laboratory animals and route of administration.
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