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Chemical Structure| 149092-50-2 Chemical Structure| 149092-50-2

Structure of AG-825
CAS No.: 149092-50-2

Chemical Structure| 149092-50-2

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AG-825 is a selective, ATP-competitive inhibitor of tyrosine phosphorylation of ErbB2 with an IC50 value of 0.35 μM. AG-825 has anti-cancer activity and significantly accelerates apoptosis of human neutrophils. It is a potential active molecule in overcoming manganese-induced neurotoxicity or Alzheimer's disease development.

Synonyms: Tyrphostin AG-825

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Product Details of AG-825

CAS No. :149092-50-2
Formula : C19H15N3O3S2
M.W : 397.47
SMILES Code : O=C(N)C(C#N)=CC1=CC(OC)=C(O)C(CSC2=NC3=CC=CC=C3S2)=C1
Synonyms :
Tyrphostin AG-825
MDL No. :MFCD01074971

Safety of AG-825

GHS Pictogram:
Signal Word:Warning
Hazard Statements:H302-H315-H319
Precautionary Statements:P501-P270-P264-P280-P302+P352-P337+P313-P305+P351+P338-P362+P364-P332+P313-P301+P312+P330

Related Pathways of AG-825

RTK
JAK-STAT
Hedgehog

Isoform Comparison

Biological Activity

In Vitro:

Cell Line
Concentration Treated Time Description References
normal cells 25, 50, 75, 100 μM 24 h To evaluate the toxicity of AG825 on normal cells, showing minimal effects on normal cells at the same concentrations. Cell Stem Cell. 2012 Sep 7;11(3):359-72
leukemia cells 25, 50, 75, 100 μM 24 h To evaluate the toxicity of AG825 on leukemia cells, showing dose-dependent eradication of leukemia cells. Cell Stem Cell. 2012 Sep 7;11(3):359-72
MCF7 cells 65 μM 5-6 days Reduced cell viability and colony formation, inhibited ErbB2-mediated signaling Cell Death Dis. 2018 Jan 19;9(2):47
human neutrophils 10 μM 6 h Accelerated neutrophil apoptosis, confirmed by Annexin-V and TO-PRO-3 staining Elife. 2019 Oct 15;8:e50990
human neutrophils 50 μM 6 h Significantly accelerated apoptosis of human neutrophils, including neutrophils from COPD patients Elife. 2019 Oct 15;8:e50990
D54-MG glioma cells 50 μM 12 h Disrupted constitutive erbB2 activation, causing a 30-mV positive shift in gBK channel activation threshold J Neurosci Res. 2005 Jul 15;81(2):179-89

In Vivo:

Species
Animal Model
Administration Dosage Frequency Description References
Mice MTLn3E xenograft tumor model Intraperitoneal injection 20 mg/kg Single injection, evaluated after 1 hour Evaluate the effect of AG825 on tumor cell intravasation, showing a significant reduction in the number of intravasating cells. Clin Cancer Res. 2009 Jun 1;15(11):3733-9
Zebrafish Tail fin injury model Incubation 10 μM 16 hours pretreatment before injury Reduced neutrophil number at the injury site and increased neutrophil apoptosis Elife. 2019 Oct 15;8:e50990

Protocol

Bio Calculators
Preparing Stock Solutions 1mg 5mg 10mg

1 mM

5 mM

10 mM

2.52mL

0.50mL

0.25mL

12.58mL

2.52mL

1.26mL

25.16mL

5.03mL

2.52mL

 

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