Cat. No.: HY-15844

AG-825

(Synonyms: Tyrphostin AG-825)

1 Cited Publications

고객리뷰

Based on 1 publication(s) in Google Scholar

AG-825 is a selective, ATP-competitive, tyrosine phosphorylation ErbB2 inhibitor with an IC₅₀ of 0.35 μM. AG825 significantly accelerates Apoptosis of human neutrophils. AG-825 increases β1AR density. AAG-825 has anticancer and anti-inflammatory activities. AAG-825 can be used in cardiovascular disease research.

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Purity: 98.13%
CAS No.: 149092-50-2
화학식: C₁₉H₁₅N₃O₃S₂
분자량:397.47

보관:

Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 2 years , -20°C, 1 year

AG-825 Chemical Structure

CAS No.: 149092-50-2

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Antibody-Drug Conjugates

One-stop solution for XDC (ADC/PDC/RDC/ApDC/FDC/ISAC/VDC/SMDC)

Biological Activity
- 제품 설명
- IC₅₀ & Target
- Cellular Effect
- In Vitro
- In Vivo
Chemical Information
Publications (1)
용액&용해도
- In Vitro
- In Vivo
순도&문서
References
Help & FAQs
Bioz

Biological Activity

제품 설명

IC₅₀ & Target^[2]

ErbB2

0.35 μM (IC₅₀)

EGFR

19 μM (IC₅₀)

All EGFR Isoforms :

All Adrenergic Receptor Isoforms :

Cellular Effect

Cell Line	Type	Value	Description	References
HCC1954	IC₅₀	30 μM Compound: AG825	Antiproliferative activity against human HCC1954 cells measured after 72 hrs by SRB assay Antiproliferative activity against human HCC1954 cells measured after 72 hrs by SRB assay	[PMID: 34844036]
NIH3T3	IC₅₀	35 μM Compound: 15	Inhibition of HER-14 (human EGFR overexpressing NIH3T3) cell proliferation Inhibition of HER-14 (human EGFR overexpressing NIH3T3) cell proliferation	[PMID: 7902440]

In Vitro

AG-825 (72 h) shows antiproliferative activity against human HCC1954 cells, with IC₅₀ of 30 μM^[6].

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

In Vivo

AG-825 (20 mg/kg, i.p.) decreases peritoneal inflammation in Zymosan (HY-159069)-treated mice, and increases lung neutrophil apoptosis and macrophage efferocytosis in a murine acute lung injury model^[4].
AG-825 (1 mg/kg, min-osmotic pump, 14 days) causes cardiac dilation and selective increase in β1AR density in mice^[7].

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

Animal Model:

Murine model of LPS induced acute lung inflammation^[4]
Dosage:

20 mg/kg
Administration:

Intraperitoneal injection (i.p.)
Result:

Had no effect on percentage of, or absolute number of neutrophils or macrophages.
Increased the percentage of neutrophil apoptosis.
Elevated macrophage efferocytosis.

Animal Model:

Murine model of Zymosan (HY-159069)-induced peritonitis^[4]
Dosage:

20 mg/kg
Administration:

Intraperitoneal injection (i.p.)
Result:

Did not induce leukopenia.
Showed fewer inflammatory cells in peritoneal lavage.
Reduced the neutrophil chemoattractant and proinflammatory cytokine, KC.
Reduced IgM.

Chemical Information

CAS No. 149092-50-2
Appearance Solid
분자량 397.47
화학식 C₁₉H₁₅N₃O₃S₂
Color Light yellow to yellow
SMILES

O=C(N)/C(C#N)=C/C1=CC(OC)=C(O)C(CSC2=NC3=CC=CC=C3S2)=C1
Synonyms

Tyrphostin AG-825
선적

Room temperature in continental US; may vary elsewhere.

보관

Powder	-20°C	3 years
	4°C	2 years
In solvent	-80°C	2 years
	-20°C	1 year

Publications (1)

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Pflugers Arch

Unlocking the potential: unveiling tyrphostins with Michael-reactive cyanoacrylate motif as promising inhibitors of human 5-lipoxygenase. [Abstract]

2024 Dec;476(12):1913-1928. PMID: 39347835

용액&용해도

In Vitro:

DMSO : 250 mg/mL (628.98 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

2.5159 mL

12.5796 mL

25.1591 mL

5 mM

0.5032 mL

2.5159 mL

5.0318 mL

10 mM

0.2516 mL

1.2580 mL

2.5159 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, 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.

몰농도 계산기

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

Mass Mass

Concentration Concentration

Volume Volume

Molecular Weight Molecular Weight

농도 희석 계산기

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

Concentration _(start) Concentration _(start)

Volume _(start) Volume _(start)

Concentration _(final) Concentration _(final)

Volume _(final) Volume _(final)

In Vivo:

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 90% (20% SBE-β-CD in Saline)

Solubility: ≥ 2.08 mg/mL (5.23 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 900 μL 20% SBE-β-CD in Saline, 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

순도&문서

Select Batch:

Purity: 99.98%

Assay: 99.98%

ee.: 99.98%

Data Sheet (279 KB)
SDS (254 KB)
- English - EN (254 KB)
- Français - FR (254 KB)
- Deutsch - DE (254 KB)
- Norwegian - NO (254 KB)
- Español - ES (254 KB)
- Swedish - SV (254 KB)
- Italian - IT (254 KB)
- Korean - KR (254 KB)
- Portuguese - PT (254 KB)
COA (2659 KB)
Elemental Analysis Report (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)
Handling Instructions (2659 KB)

References

[1]. Wolfson E, et al. Nucleolin and ErbB2 inhibition reduces tumorigenicity of ErbB2-positive breast cancer. Cell Death Dis. 2018 Jan 19;9(2):47. [Content Brief]

[2]. Gazit A, et al. Tyrphostins. 3. Structure-activity relationship studies of alpha-substituted benzylidenemalononitrile 5-S-aryltyrphostins. J Med Chem. 1993 Nov 12;36(23):3556-64. [Content Brief]

[3]. He H, et al. Signal therapy for RAS-induced cancers in combination of AG 879 and PP1, specific inhibitors for ErbB2 and Src family kinases, that block PAK activation. Cancer J. 2001 May-Jun;7(3):191-202. [Content Brief]

[4]. Rahman A, et al. Inhibition of ErbB kinase signalling promotes resolution of neutrophilic inflammation. Elife. 2019 Oct 15;8. pii: e50990. [Content Brief]

[5]. Ling J, et al. Identifying key genes, pathways and screening therapeutic agents for manganese-induced Alzheimer disease using bioinformatics analysis. Medicine (Baltimore). 2018 Jun;97(22):e10775. [Content Brief]

[6]. Piven YA, et al. Novel O-acylated (E)-3-aryl-6,7-dihydrobenzisoxazol-4(5H)-one oximes targeting HSP90-HER2 axis in breast cancer cells. Bioorg Med Chem. 2022 Jan 1;53:116521. [Content Brief]

[7]. Gupta MK, et al. Anthracycline Cardiotoxicity Is Associated With Elevated β1-Adrenergic Receptor Density. J Am Heart Assoc. 2022 Feb 15;11(4):e023457. [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, 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	1 mM	2.5159 mL	12.5796 mL	25.1591 mL	62.8978 mL
	5 mM	0.5032 mL	2.5159 mL	5.0318 mL	12.5796 mL
	10 mM	0.2516 mL	1.2580 mL	2.5159 mL	6.2898 mL
	15 mM	0.1677 mL	0.8386 mL	1.6773 mL	4.1932 mL
	20 mM	0.1258 mL	0.6290 mL	1.2580 mL	3.1449 mL
	25 mM	0.1006 mL	0.5032 mL	1.0064 mL	2.5159 mL
	30 mM	0.0839 mL	0.4193 mL	0.8386 mL	2.0966 mL
	40 mM	0.0629 mL	0.3145 mL	0.6290 mL	1.5724 mL
	50 mM	0.0503 mL	0.2516 mL	0.5032 mL	1.2580 mL
	60 mM	0.0419 mL	0.2097 mL	0.4193 mL	1.0483 mL
	80 mM	0.0314 mL	0.1572 mL	0.3145 mL	0.7862 mL
	100 mM	0.0252 mL	0.1258 mL	0.2516 mL	0.6290 mL

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AG-825

Apoptosis Compound Library

GPCR/G Protein Compound Library

Immunology/Inflammation Compound Library

JAK/STAT Compound Library

Kinase Inhibitor Library

Neuronal Signaling Compound Library

Protein Tyrosine Kinase Compound Library

Anti-Cancer Compound Library

Covalent Screening Library

Differentiation Inducing Compound Library

Anti-Cardiovascular Disease Compound Library

Neurotransmitter Receptor Compound Library

Anti-Hepatitis C Virus Compound Library

Anti-Breast Cancer Compound Library

Anti-Lung Cancer Compound Library

Anti-Pancreatic Cancer Compound Library

Anti-Obesity Compound Library

Angiogenesis-Related Compound Library

Anti-Liver Cancer Compound Library

Anti-Colorectal Cancer Compound Library

Antidepressant Compound Library

Anti-Prostate Cancer Compound Library

Cancer Stem Cells Compound Library

Heterocyclic Compound Library

Membrane Protein-targeted Compound Library

Membrane Receptor-targeted Compound Library

Cysteine Targeted Covalent Library

Highly Selective Inhibitors Library

Highly Selective Activators Library

Cytokine Inhibitors Library

Cell Death Library

Anti-Ovarian Cancer Compound Library

Multi-Target Compound Library

Bioactive Compound Library Max

MCE Bioactive Compound Library

Covalent Screening Library Plus

Bioactive Compound Library

Anti-Gastric Cancer Compound Library

Anti-Brain Cancer Compound Library

Protein Kinase Compound Library

Non-Alcoholic Fatty Liver Disease (NAFLD) Compound Library

Cell Proliferation Compound Library

High-Throughput Bioactive Compound Library

Posttranslational Modification Library

Lactylation Compound Library

Publications Citing Use of MedChemExpress (MCE) AG-825

All EGFR Isoforms

All Adrenergic Receptor Isoforms

Biological Activity

Chemical Information

Publications (1)

용액&용해도

순도&문서

References

Help & FAQs

Complete Stock Solution Preparation Table

AG-825 Related Classifications

Cat. No.: HY-15844