1. Apoptosis
    Metabolic Enzyme/Protease
  2. MDM-2/p53
    E1/E2/E3 Enzyme
    Apoptosis
  3. APG-115

APG-115 (Synonyms: AA-115)

Cat. No.: HY-101518 Purity: 98.16%
Handling Instructions

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

For research use only. We do not sell to patients.

APG-115 Chemical Structure

APG-115 Chemical Structure

CAS No. : 1818393-16-6

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1 mg USD 550 In-stock
Estimated Time of Arrival: December 31
5 mg USD 980 In-stock
Estimated Time of Arrival: December 31
10 mg USD 1500 In-stock
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Based on 1 publication(s) in Google Scholar

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Description

APG-115 (AA-115) is an orally active MDM2 protein inhibitor binding to MDM2 protein with IC50 and Ki values of 3.8 nM and 1 nM, respectively[1]. APG-115 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]

In Vitro

APG-115 (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].
APG-115 (0.02 μM, 0.2 μM; 48 hours) enhances the anti-proliferative effect of radiotherapy at different radiation dose[3].
APG-115 (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].
APG-115 (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].
APG-115 (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].

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.
In Vivo

APG-115 (Delivered orally; 100 mg/kg; once daily; 10 days) enhances radiation antitumor effect in gastric adenocarcinoma in vivo[3].

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.
Clinical Trial
Molecular Weight

642.59

Formula

C₃₄H₃₈Cl₂FN₃O₄

CAS No.

1818393-16-6

SMILES

O=C(N1)[[email protected]]([[email protected]@H](C(C=CC=C2Cl)=C2F)[[email protected]@H]3C(NC45CCC(C(O)=O)(CC5)CC4)=O)(C(C1=C6)=CC=C6Cl)C7(CCCCC7)N3CC

Shipping

Room temperature in continental US; may vary elsewhere.

Storage
Powder -20°C 3 years
  4°C 2 years
In solvent -80°C 6 months
  -20°C 1 month
Solvent & Solubility
In Vitro: 

DMSO : 100 mg/mL (155.62 mM; Need ultrasonic)

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
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.
In Vivo:
  • 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

  • 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

  • 3.

    Add each solvent one by one:  10% DMSO    90% corn oil

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

*All of the co-solvents are provided by MCE.
References
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Keywords:

APG-115AA-115APG115APG 115AA115AA 115MDM-2/p53E1/E2/E3 EnzymeApoptosisE1 activating enzymeE2 conjugating enzymeE3 ligating enzymeUbiquitin activating enzymeUbiquitin conjugating enzymeUbiquitin ligaseInhibitorinhibitorinhibit

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Product Name:
APG-115
Cat. No.:
HY-101518
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