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AGX51 

Cat. No.: HY-129241 Purity: 99.09%
COA Handling Instructions

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
Solution
10 mM * 1 mL in DMSO USD 332 In-stock
Oil + Solvent
10 mM * 1 mL
ready for reconstitution
 USD 332 In-stock
Oil
5 mg USD 350 In-stock
10 mg USD 550 In-stock
25 mg USD 990 In-stock
50 mg USD 1650 In-stock
100 mg USD 2250 In-stock
200 mg   Get quote  
500 mg   Get quote  

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

Customer Review

Based on 2 publication(s) in Google Scholar

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  • Purity & Documentation

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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].

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].

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

Appearance

Oil

Formula

C27H29NO4
CAS No.
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 6 months
-20°C 1 month
Solvent & Solubility
In Vitro: 

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

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
10 mM 0.2317 mL 1.1587 mL 2.3174 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: ≥ 2.08 mg/mL (4.82 mM); Clear solution

  • 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

  • 3.

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

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

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

Purity: 99.09%

COA (257 KB) HNMR (281 KB) LCMS (97 KB)

Handling Instructions (2659 KB)
References
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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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Keywords:

AGX51330834-54-3AGX 51AGX-51Othersanti-tumorTNBCubiquitinhelix-loop-helixInhibitorinhibitorinhibit

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