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AGX51 is a first-in-class pan-Id (inhibitors of DNA-binding/differentiation proteins) antagonist and degrader. AGX51 inhibits the Id1-E47 interaction, leading to ubiquitin-mediated degradation of Ids, cell growth arrest, and reduces viability. AGX51 inhibits the TNBC cell lines with IC50s of nearly 25 μM. AGX51 can be used for the research of cancer.

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

AGX51 Chemical Structure

AGX51 Chemical Structure

CAS No. : 330834-54-3

Size Price Stock Quantity
Oil + Solvent
10 mM * 1 mL in DMSO
ready for reconstitution
USD 308 In-stock
Solution
10 mM * 1 mL in DMSO USD 308 In-stock
Oil
5 mg USD 280 In-stock
10 mg USD 450 In-stock
25 mg USD 880 In-stock
50 mg USD 1400 In-stock
100 mg USD 1950 In-stock
200 mg   Get quote  
500 mg   Get quote  

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Customer Review

Based on 3 publication(s) in Google Scholar

Top Publications Citing Use of Products
  • Biological Activity

  • Purity & Documentation

  • References

  • Customer Review

Description

AGX51 is a first-in-class pan-Id (inhibitors of DNA-binding/differentiation proteins) antagonist and degrader. AGX51 inhibits the Id1-E47 interaction, leading to ubiquitin-mediated degradation of Ids, cell growth arrest, and reduces viability. AGX51 inhibits the TNBC cell lines with IC50s of nearly 25 μM. AGX51 can be used for the research of cancer[1].

IC50 & Target

IC50: 26.66 μM (4T1), 8.7 μM (HMLE RAS Twist), 22.28 μM (MDA-MB-157), 30.91 μM (MDA-MB-436), 36.55 μM (SK-BR-3), 60 μM (MCF-7), 10.89 μM (PDX-BR7), 11.97 μM (PDX-IBT) , 18.56 μM (PDX-BR11)[1]

In Vitro

AGX51 (0-80 μM; 24 h) decreases ID1 protein levels in 4T1 cells[1].
AGX51 (40 μM; 0-72 h) decreases ID1 levels protein with a 40 μM concentratio in 4T1 cells[1].
AGX51 (40 μM; 24 h) influences 4T1 cells , ER+, HER2+, TNBC and three breast cancer PDX cell ines[1].
AGX51 (0-80 μM; 24-48 h) influences cell cycle of 4T1 cells[1].
AGX51 (40 μM; 4-24 h) influences phospho-histone H3 levels in 4T1 cells[1].
AGX51 (40 μM; 24 h) influences ROS levels in 4T1 cells[1].

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

Western Blot Analysis[1]

Cell Line: 4T1 cells
Concentration: 0, 5, 10, 20, 40 and 80 μM
Incubation Time: 24 hours
Result: Decreased ID1 protein levels starting at a concentration of 40 μM in 4T1 cells.

Western Blot Analysis[1]

Cell Line: 4T1 cells
Concentration: 40 μM
Incubation Time: 0, 2, 4, 8 , 12, 24, 48 and 72 hours
Result: Decreased ID1 protein levels starting at 4 h, while until 24 h ID1 protein completely loss.

Cell Viability Assay[1]

Cell Line: 4T1 cells, HMLE RAS Twist, MDA-MB-157, MDA-MB-436, MDA-MB-231, MDA-MB-453, BT-474, MDA-MB-361, SK-BR-3, MCF-7, T47-D, PDX-BR7, PDX-IBT and PDX-BR11
Concentration: 40 μM
Incubation Time: 24 hours
Result: Inhibited 4T1, HMLE RAS Twist, MDA-MB-157, MDA-MB-436, SK-BR-3, MCF-7, PDX-BR7, PDX-IBT and PDX-BR11 cell lines with IC50s of 26.66, 8.7, 22.28, 30.91, 36.55, 60, 10.89, 11.97 and 18.56 μM, respectively.

Cell Cycle Analysis[1]

Cell Line: 4T1 cells
Concentration: 40 μM
Incubation Time: 24 and 48 hours
Result: Affected cell cycle of 4T1 cells with a G0/G1 phase accumulation.

Cell Viability Assay[1]

Cell Line: 4T1 cells
Concentration: 40 μM
Incubation Time: 4 and 24 hours
Result: Reduced phospho-histone H3 levels in 4T1 cells.

Cell Viability Assay[1]

Cell Line: 4T1 cells
Concentration: 40 μM
Incubation Time: 24 hours
Result: Increased ROS level of 4T1 cells and indicated ROS production is a main mechanism of cell killing.
In Vivo

AGX51 (50 mg/kg; i.p. twice a day for 4 weeks) inhibits lung metastasis[1].
AGX51 (15 mg/kg; i.p. twice a day for 3 weeks) exibits anti-tumor activity with autochronous cancer[1].

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

Animal Model: Balb/c mice with luciferase-labeled 4T1 cells[1]
Dosage: 50 mg/kg
Administration: Intraperitoneal injection; 60 mg/kg twice a day; for 4 weeks
Result: Inhibited lung metastasis development.
Animal Model: A/J mice with AOM colon tumor model[1]
Dosage: 15 mg/kg
Administration: Intraperitoneal injection; 15 mg/kg twice a day; for 3 weeks
Result: Dreased the colon tumors and exhibited anti-tumor activity in AOM colon tumor mice.
Molecular Weight

431.52

Formula

C27H29NO4

CAS No.
Appearance

Oil

Color

Light yellow to yellow

SMILES

CCC(N(CCC(C1=CC=C(OCO2)C2=C1)C3=CC=CC=C3OC)CC4=CC=CC=C4)=O

Shipping

Room temperature in continental US; may vary elsewhere.

Storage
Pure form -20°C 3 years
4°C 2 years
In solvent -80°C 2 years
-20°C 1 year
Solvent & Solubility
In Vitro: 

DMSO : 100 mg/mL (231.74 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

Ethanol : 100 mg/mL (231.74 mM; Need ultrasonic)

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 2.3174 mL 11.5869 mL 23.1739 mL
5 mM 0.4635 mL 2.3174 mL 4.6348 mL
View the Complete Stock Solution Preparation Table

* 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, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.

  • Molarity Calculator

  • Dilution Calculator

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

Mass
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Concentration
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Volume
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Molecular Weight *

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

This equation is commonly abbreviated as: C1V1 = C2V2

Concentration (start)

C1

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Volume (start)

V1

=
Concentration (final)

C2

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Volume (final)

V2

In Vivo:

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

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: ≥ 2.08 mg/mL (4.82 mM); Clear solution

    This protocol yields a clear solution of ≥ 2.08 mg/mL (saturation unknown).

    Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (20.8 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.

    Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
  • Protocol 2

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

    Solubility: 2.08 mg/mL (4.82 mM); Suspended solution; Need ultrasonic

    This protocol yields a suspended solution of 2.08 mg/mL. Suspended solution can be used for oral and intraperitoneal injection.

    Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (20.8 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.

    Preparation of 20% SBE-β-CD in Saline (4°C, storage for one week): 2 g SBE-β-CD powder is dissolved in 10 mL Saline, completely dissolve until clear.
In Vivo Dissolution Calculator
Please enter the basic information of animal experiments:

Dosage

mg/kg

Animal weight
(per animal)

g

Dosing volume
(per animal)

μL

Number of animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
%
DMSO +
+
%
Tween-80 +
%
Saline
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
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).
Calculation results:
Working solution concentration: mg/mL
Method for preparing stock solution: mg drug dissolved in μL  DMSO (Stock solution concentration: mg/mL).
The concentration of the stock solution you require exceeds the measured solubility. The following solution is for reference only. If necessary, please contact MedChemExpress (MCE).
Method for preparing in vivo working solution for animal experiments: Take μL DMSO stock solution, add μL . μL , mix evenly, next add μL Tween 80, mix evenly, then add μL Saline.
 If the continuous dosing period exceeds half a month, please choose this protocol carefully.
Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.
Purity & Documentation

Purity: 99.09%

References

Complete Stock Solution Preparation Table

* 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, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.

Optional Solvent Concentration Solvent Mass 1 mg 5 mg 10 mg 25 mg
DMSO / Ethanol 1 mM 2.3174 mL 11.5869 mL 23.1739 mL 57.9347 mL
5 mM 0.4635 mL 2.3174 mL 4.6348 mL 11.5869 mL
10 mM 0.2317 mL 1.1587 mL 2.3174 mL 5.7935 mL
15 mM 0.1545 mL 0.7725 mL 1.5449 mL 3.8623 mL
20 mM 0.1159 mL 0.5793 mL 1.1587 mL 2.8967 mL
25 mM 0.0927 mL 0.4635 mL 0.9270 mL 2.3174 mL
30 mM 0.0772 mL 0.3862 mL 0.7725 mL 1.9312 mL
40 mM 0.0579 mL 0.2897 mL 0.5793 mL 1.4484 mL
50 mM 0.0463 mL 0.2317 mL 0.4635 mL 1.1587 mL
60 mM 0.0386 mL 0.1931 mL 0.3862 mL 0.9656 mL
80 mM 0.0290 mL 0.1448 mL 0.2897 mL 0.7242 mL
100 mM 0.0232 mL 0.1159 mL 0.2317 mL 0.5793 mL
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AGX51 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.

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