AG-825

Names

[ Name ]:
AG-825

[Synonym ]:
2-Propenamide, 3-[3-[(2-benzothiazolylthio)methyl]-4-hydroxy-5-methoxyphenyl]-2-cyano-, (2E)-
(2E)-3-{3-[(1,3-Benzothiazol-2-ylsulfanyl)methyl]-4-hydroxy-5-methoxyphenyl}-2-cyanoacrylamide
TYRPHOSTIN C15
(2E)-3-{3-[(1,3-benzothiazol-2-ylsulfanyl)methyl]-4-hydroxy-5-methoxyphenyl}-2-cyanoprop-2-enamide
5-[(Benzothiazol-2-yl)thiomethyl]-4-hydroxy-3-methoxybenzylidenecyanoacetamide Tyrphostin C15

Biological Activity

[Description]:

AG-825 (Tyrphostin AG-825) is a selective and ATP-competitive ErbB2 inhibitor which suppresses tyrosine phosphorylation, with an IC50 of 0.35 μM. AG-825 displays anti-cancer activity[1][2][3]. AG825 significantly accelerates apoptosis of human neutrophils[4]. AG-825 is a potential agent for overcoming Mn-induced neurotoxicity or AD development[5].

[Related Catalog]:

Signaling Pathways >> Apoptosis >> Apoptosis

Research Areas >> Cancer

Signaling Pathways >> JAK/STAT Signaling >> EGFR

Signaling Pathways >> Protein Tyrosine Kinase/RTK >> EGFR

[Target]

ErbB2:0.35 μM (IC50)

EGFR:19 μM (IC50)

[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.

[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.

[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.

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

[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.

Chemical & Physical Properties

[ Density]:
1.5±0.1 g/cm3

[ Boiling Point ]:
689.3±65.0 °C at 760 mmHg

[ Molecular Formula ]:
C₁₉H₁₅N₃O₃S₂

[ Molecular Weight ]:
397.471

[ Flash Point ]:
370.7±34.3 °C

[ Exact Mass ]:
397.055481

[ PSA ]:
162.77000

[ LogP ]:
2.89

[ Vapour Pressure ]:
0.0±2.2 mmHg at 25°C

[ Index of Refraction ]:
1.733

[ Storage condition ]:
−20°C

[ Water Solubility ]:
DMSO: soluble

MSDS

Click to get detail MSDS

Safety Information

[ Personal Protective Equipment ]:
Eyeshields;Gloves;type N95 (US);type P1 (EN143) respirator filter

[ Safety Phrases ]:
22-24/25

[ RIDADR ]:
NONH for all modes of transport

[ WGK Germany ]:
3

Articles

Endogenous expression of the sodium iodide symporter mediates uptake of iodide in murine models of colorectal carcinoma.

Int. J. Cancer 125(12) , 2783-91, (2009)

The sodium iodide symporter (NIS) mediates iodide uptake into the thyroid. Because of this mechanism, differentiated thyroid cancer is susceptible for radioiodine therapy. Functional NIS expression in...

Degradation of HER2 receptor through hypericin-mediated photodynamic therapy.

Photochem. Photobiol. 86 , 200-5, (2010)

Current treatment of breast cancer is often affected by resistance to therapeutics, for which the human epidermal growth factor receptor 2 (HER2) may be responsible. Here, we report for the first time...