Powder: -20°C for 3 years | In solvent: -80°C for 1 year
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.
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 |
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 |
Powder: -20°C for 3 years | In solvent: -80°C for 1 year
DMSO: 90 mg/mL (140.1 mM), Sonification is recommended.
You can also refer to dose conversion for different animals. More
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Alrizomadlin 1818393-16-6 Apoptosis Mdm2 AA 115 APG-115 APG115 AA115 APG 115 AA-115 inhibitor inhibit