製品番号: HY-101518

Alrizomadlin

(別名: APG-115; AA-115)

4 Cited Publications

カスタマーレビュー

Based on 4 publication(s) in Google Scholar

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

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研究用途以外に使用した場合、当社は一切の責任を負いかねます。

純度: 99.89%
CAS 番号: 1818393-16-6
分子式: C₃₄H₃₈Cl₂FN₃O₄
分子量:642.59

保管条件:

Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 6 months , -20°C, 1 month

Alrizomadlin 構造式

CAS 番号: 1818393-16-6

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数量

Amount: USD 0.00

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生物活性
- 製品説明
- IC₅₀ & Target
- Cellular Effect
- 体外実験
- 体内実験
- 臨床実験
化学情報
Publications (4)
溶剤 & 溶解度
- 体外
- 体内
純度とドキュメンテーション
参考文献
Help & FAQs
関連分類
Bioz

生物活性

製品説明

Alrizomadlin (APG-115) is an orally active MDM2 protein inhibitor binding to MDM2 protein with IC₅₀ and K_i 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].

IC₅₀ & Target

IC50: 3.8 nm (APG-115)^[1]

Cellular Effect

Cell Line	Type	Value	Description	References
HCT-116	IC₅₀	104 nM Compound: 60	Cytotoxicity against wild type p53 expressing human HCT116 cells assessed as cell growth inhibition by WST8 assay Cytotoxicity against wild type p53 expressing human HCT116 cells assessed as cell growth inhibition by WST8 assay	[PMID: 28339198]
HCT-116	IC₅₀	8 μM Compound: 60	Cytotoxicity against p53 deficient human HCT116 cells assessed as cell growth inhibition by WST8 assay Cytotoxicity against p53 deficient human HCT116 cells assessed as cell growth inhibition by WST8 assay	[PMID: 28339198]
LNCaP	IC₅₀	18 nM Compound: 60	Cytotoxicity against wild type p53 expressing human LNCAP cells assessed as cell growth inhibition by WST8 assay Cytotoxicity against wild type p53 expressing human LNCAP cells assessed as cell growth inhibition by WST8 assay	[PMID: 28339198]
PC-3	IC₅₀	22 μM Compound: 60	Cytotoxicity against p53 deficient human PC3 cells assessed as cell growth inhibition by WST8 assay Cytotoxicity against p53 deficient human PC3 cells assessed as cell growth inhibition by WST8 assay	[PMID: 28339198]
RS4-11	IC₅₀	38 nM Compound: 60	Cytotoxicity against wild type p53 expressing human RS4:11 cells assessed as cell growth inhibition by WST8 assay Cytotoxicity against wild type p53 expressing human RS4:11 cells assessed as cell growth inhibition by WST8 assay	[PMID: 28339198]
SAOS-2	IC₅₀	22.7 μM Compound: 60	Cytotoxicity against p53 deficient human Saos2 cells assessed as cell growth inhibition by WST8 assay Cytotoxicity against p53 deficient human Saos2 cells assessed as cell growth inhibition by WST8 assay	[PMID: 28339198]
SJSA-1	IC₅₀	0.06 μM Compound: 60	Cytotoxicity against p53 expressing human SJSA1 cells assessed as cell growth inhibition by WST8 assay Cytotoxicity against p53 expressing human SJSA1 cells assessed as cell growth inhibition by WST8 assay	[PMID: 28339198]

体外実験

Alrizomadlin (0.001-100 μM; 72 hours) inhibits cell proliferation in concentration-dependent manner, with IC₅₀s of 18.9 ± 15.6 nM and 103.5 ± 18.3 nM respectively in AGS and MKN45 cells^[3].
Alrizomadlin (0.02 μM, 0.2 μM; 48 hours) enhances the anti-proliferative effect of radiotherapy at different radiation dose^[3].
Alrizomadlin (0.02 μM, 0.2 μM; 48 hours) affects progression by inducing cells arrested at G0/G1 phase in AGS and MKN45 cell with wild p53^[3].
Alrizomadlin (0.02 μM, 0.2 μM; 24 hours) activates p53 to enhance radiosensitivity in AGS and MKN45 cells; stable knockout of p53 abrogates expression of MDM2, p53, p21, PUMA, BAX, Cleaved-caspase3, γH2AX^[3].
Alrizomadlin (0.3 μM, 1 μM, 3 μM, 10 μM; 24 hours) leads to a concentration-dependent cell cycle arrest in G2/M phases and a decreasing in S-phase in p53 wide-type cell lines (TPC-1, KTC-1)^[4].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Cell Proliferation Assay^[3]

Cell Line:

AGS and MKN45 cells
Concentration:

0.0001 μM, 0.001 μM, 0.01 μM, 0.1 μM, 1 μM, 10 μM, 100 μM
Incubation Time:

72 hours
Result:

Inhibited cell proliferation in a concentration-dependent manner.

RT-PCR^[3]

Cell Line:

AGS and MKN45 cells
Concentration:

0.02 μM, 0.2 μM
Incubation Time:

48 hours
Result:

Elevated MDM2, p21, PUMA and BAX mRNA expression.

Cell Cycle Analysis^[3]

Cell Line:

AGS and MKN45 cells
Concentration:

0.02 μM, 0.2 μM
Incubation Time:

48 hours
Result:

Arrested cells at G0/G1 phase.

Apoptosis Analysis^[4]

Cell Line:

DePTC p53 wide-type cell line: TPC-1 cells, KTC-1 cells
Concentration:

0.3μM, 1μM, 3μM, 10 μM
Incubation Time:

24 hours
Result:

Reduced cell population in S-phase, whereas accumulation of cells at G2/M phases.

Western Blot Analysis^[3]

Cell Line:

AGS and MKN45 cells
Concentration:

0.2 μM
Incubation Time:

72 hours
Result:

Enhanced expressions of MDM2 and p53, stable knockout of p53 abrogated them.

体内実験

Alrizomadlin (Delivered orally; 100 mg/kg; once daily; 10 days) enhances radiation antitumor effect in gastric adenocarcinoma in vivo^[3].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model:

Four-week-old male BALB/c athymic nude mice with MKN45 cells^[3]
Dosage:

100 mg/kg
Administration:

Deliverer orally; once daily; 10 days
Result:

Decreased xenograft tumor growth.

臨床実験

NCT Number	Sponsor	Condition	Start Date	Phase A549
NCT01329991	Plexxikon\|		2011-05	PHASE1

化学情報

CAS 番号 1818393-16-6
性状 Solid
分子量 642.59
分子式 C₃₄H₃₈Cl₂FN₃O₄
Color White to off-white
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
別名

APG-115; AA-115
輸送条件

Room temperature in continental US; may vary elsewhere.

保管条件

Powder	-20°C	3 years
	4°C	2 years
In solvent	-80°C	6 months
	-20°C	1 month

Publications (4)

All RT-PCRWB

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Journal Impact Factor

Redox Biol

p53 and fatty acids collaborate to trigger ferroptosis via the FBXO2-FABP5 axis in colorectal cancer. [Abstract]

2026 Mar:90:104043. PMID: 41604941

Alrizomadlin purchased from MedChemExpress. Usage Cited in: Redox Biol. 2026 Mar:90:104043. [Abstract]

RKO cells treated with or without 5-fluorouracil (5-FU, 40 μM), Etoposide (20 μM), Nutlin-3 (20 μM), or Alrizomadlin (APG-115, 2 μM) for 24 h.
Cell Death Differ

p53 transcriptionally activates DCP1B to suppress tumor progression and enhance tumor sensitivity to PI3K blockade in non-small cell lung cancer. [Abstract]

2025 Apr 9. PMID: 40200093
Cell Rep

Loss of p53 exacerbates autoimmunity by reprogramming propionyl-CoA metabolism and histone modifications in Treg cells. [Abstract]

2026 Mar 15;45(3):117084. PMID: 41838722

Alrizomadlin purchased from MedChemExpress. Usage Cited in: Cell Rep. 2026 Mar 15;45(3):117084. [Abstract]

Western blot analysis of CD4+CD25+YFP+ Treg cells isolated from Foxp3Cre and Foxp3CreTrp53fl/fl mice and treated with APG-115 (Alrizomadlin: 0, 1, 5, and 10 μM) for 24 h.
Cells

PROTAC-Mediated Targeted Degradation of MDM2 Induces Tumor-Suppressive Signaling in Osteosarcoma Cells. [Abstract]

2026 Mar 5;15(5):473. PMID: 41827906

溶剤 & 溶解度

体外:

DMSO : 100 mg/mL (155.62 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

View the Complete Stock Solution Preparation Table

Preparing Stock Solutions

View the Complete Stock Solution Preparation Table

Concentration Solvent Mass

1 mg

5 mg

10 mg

Concentration

Solvent

Mass

1 mM

1.5562 mL

7.7810 mL

15.5620 mL

5 mM

0.3112 mL

1.5562 mL

3.1124 mL

10 mM

0.1556 mL

0.7781 mL

1.5562 mL

Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.

Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

モル濃度計算機

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

Mass Mass

濃度濃度

体積体積

分子量分子量

希釈計算機

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体積 _(開始) 体積 _(開始)

濃度 _(終了) 濃度 _(終了)

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体内:

Select the appropriate dissolution method based on your experimental animal and administration route.

Stock Solution Working Solution

For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for In Vivo experiments, it is recommended to prepare freshly and use it on the same day.
The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.

Protocol 1

Add each solvent one by one: 10% DMSO 40% PEG300 5% Tween-80 45% Saline

Solubility: ≥ 5 mg/mL (7.78 mM); Clear solution

This protocol yields a clear solution of ≥ 5 mg/mL (saturation unknown).

Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (50.0 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.

Protocol 2

Add each solvent one by one: 10% DMSO 90% (20% SBE-β-CD in Saline)

Solubility: ≥ 5 mg/mL (7.78 mM); Clear solution

This protocol yields a clear solution of ≥ 5 mg/mL (saturation unknown).

Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (50.0 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.

Protocol 3

Add each solvent one by one: 10% DMSO 90% Corn Oil

Solubility: ≥ 2.5 mg/mL (3.89 mM); Clear solution

This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown). If the continuous dosing period exceeds half a month, please choose this protocol carefully.

Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 900 μL Corn oil, and mix evenly.

In Vivo Dissolution Calculator

Please enter the basic information of animal experiments:

Dosage Dosage
mg/kg
Animal Weight (Per Animal) Animal Weight (Per Animal)
g
Dosing Volume (Per Animal) Dosing Volume (Per Animal)
μL
Number of Animals Number of Animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Please enter your animal formula composition:

%
DMSO +

Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
%
+
+
%
Tween-80 + +
%
Saline +

The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).

Working solution concentration: 0.22 mg/mL

純度とドキュメンテーション

バッチを選択:

純度: 99.98%

Assay: 99.98%

ee.: 99.98%

データシート (286 KB)
SDS (254 KB)
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- Portuguese - PT (254 KB)
COA (2659 KB)
元素分析報告書 (2659 KB)
HNMR (2659 KB)
CNMR (2659 KB)
RP-HPLC (2659 KB)
NP-HPLC (2659 KB)
MS (2659 KB)
LCMS (2659 KB)
IR (2659 KB)
GC (2659 KB)
OR (2659 KB)
SDS-PAGE (2659 KB)
SEC-HPLC (2659 KB)
Other Report (2659 KB)
取扱説明書 (2659 KB)

参考文献

[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. [Content Brief]

[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. [Content Brief]

Help & FAQs

How should lyophilized recombinant proteins be reconstituted and stored?

1. Before opening the cap, centrifuge the vial at 13000 rpm for 20-30 seconds. This step will ensure that any lyophilized powder that may have adhered to the cap or walls is collected at the bottom of the vial, minimizing the risk of product loss.

Complete Stock Solution Preparation Table

Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

Optional Solvent	Concentration Solvent Mass	1 mg	5 mg	10 mg	25 mg
DMSO	1 mM	1.5562 mL	7.7810 mL	15.5620 mL	38.9051 mL
	5 mM	0.3112 mL	1.5562 mL	3.1124 mL	7.7810 mL
	10 mM	0.1556 mL	0.7781 mL	1.5562 mL	3.8905 mL
	15 mM	0.1037 mL	0.5187 mL	1.0375 mL	2.5937 mL
	20 mM	0.0778 mL	0.3891 mL	0.7781 mL	1.9453 mL
	25 mM	0.0622 mL	0.3112 mL	0.6225 mL	1.5562 mL
	30 mM	0.0519 mL	0.2594 mL	0.5187 mL	1.2968 mL
	40 mM	0.0389 mL	0.1945 mL	0.3891 mL	0.9726 mL
	50 mM	0.0311 mL	0.1556 mL	0.3112 mL	0.7781 mL
	60 mM	0.0259 mL	0.1297 mL	0.2594 mL	0.6484 mL
	80 mM	0.0195 mL	0.0973 mL	0.1945 mL	0.4863 mL
	100 mM	0.0156 mL	0.0778 mL	0.1556 mL	0.3891 mL

Keywords

Alrizomadlin

4 Cited Publications

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Alrizomadlin

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MedChemExpress（MCE）の使用を引用している文献 Alrizomadlin

生物活性

化学情報

Publications (4)

溶剤 & 溶解度

純度とドキュメンテーション

参考文献

Help & FAQs

Complete Stock Solution Preparation Table

Alrizomadlin 関連分類

HY-101518 関連分類