2. Apoptosis Metabolic Enzyme/Protease
  3. MDM-2/p53 E1/E2/E3 Enzyme Apoptosis
  4. Alrizomadlin

Alrizomadlin  (Synonyms: APG-115; AA-115)

Cat. No.: HY-101518 Purity: 98.31%
COA Handling Instructions

Alrizomadlin (APG-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. Alrizomadlin 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.

Alrizomadlin Chemical Structure

Alrizomadlin Chemical Structure

CAS No. : 1818393-16-6

Size Price Stock Quantity
Solution
10 mM * 1 mL in DMSO USD 1060 In-stock
Solid + Solvent
10 mM * 1 mL
ready for reconstitution
 USD 1060 In-stock
Solid
1 mg USD 320 In-stock
5 mg USD 750 In-stock
10 mg USD 1200 In-stock
50 mg USD 3600 In-stock
100 mg USD 5400 In-stock
200 mg   Get quote  
500 mg   Get quote  

* Please select Quantity before adding items.

This product is a controlled substance and not for sale in your territory.

Customer Review

Based on 1 publication(s) in Google Scholar

Alrizomadlin Related Antibodies

Top Publications Citing Use of Products

  • Biological Activity

  • Purity & Documentation

  • References

  • Customer Review

Description

Alrizomadlin (APG-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]. 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]
In Vitro

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].

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

Alrizomadlin Related Antibodies

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

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

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.
Clinical Trial
Molecular Weight

642.59

Appearance

Solid

Formula

C34H38Cl2FN3O4
CAS No.
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
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: ≥ 2.5 mg/mL (3.89 mM); Clear solution

*All of the co-solvents are available by MCE.
Purity & Documentation

Purity: 98.31%

COA (259 KB) HNMR (278 KB) LCMS (87 KB)

Handling Instructions (2659 KB)
References
  • No file chosen (Maximum size is: 1024 Kb)
  • If you have published this work, please enter the PubMed ID.
  • Your name will appear on the site.

Alrizomadlin Related Classifications

Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

  • Molarity Calculator

  • Dilution Calculator

The molarity calculator equation

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

Mass   Concentration   Volume   Molecular Weight *
= × ×

The dilution calculator equation

Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

This equation is commonly abbreviated as: C1V1 = C2V2

Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
× = ×
C1   V1   C2   V2

Keywords:

Alrizomadlin1818393-16-6APG-115 AA-115APG115APG 115AA115AA 115AA-115MDM-2/p53E1/E2/E3 EnzymeApoptosisE1 activating enzymeE2 conjugating enzymeE3 ligating enzymeUbiquitin activating enzymeUbiquitin conjugating enzymeUbiquitin ligaseInhibitorinhibitorinhibit

Your Recently Viewed Products:

Inquiry Online

Your information is safe with us. * Required Fields.

Product Name

  

Salutation

Applicant Name *

 

Email Address *

Phone Number *

 

Organization Name *

Department *

 

Requested quantity *

Country or Region *

      

Remarks

Bulk Inquiry

Inquiry Information

Product Name:
Alrizomadlin
Cat. No.:
HY-101518
Quantity:
MCE Japan Authorized Agent:

Customer Review

Thank You for Your Feedback!

Request for HNMR Report

Please fill out this form to request the QC report. We will send it to your Email address shortly.

Your information is safe with us. * Required Fields.

Product Name

  

Lot #

Applicant Name *

 

Email Address *

Phone Number

 

Department *

Organization Name *

 

Country or Region *

Remarks

Request for HNMR Report

We have received your request and will respond to you as soon as possible.