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Chemical Structure| 148741-30-4 Chemical Structure| 148741-30-4

Structure of Tyrphostin AG 879
CAS No.: 148741-30-4

Chemical Structure| 148741-30-4

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Tyrphostin AG 879 potently inhibits HER2/ErbB2 with IC50 of 1 μM, 100- and 500-fold higher selective to ErbB2 than PDGFR and EGFR.

Synonyms: AG 879

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Product Details of Tyrphostin AG 879

CAS No. :148741-30-4
Formula : C18H24N2OS
M.W : 316.46
SMILES Code : S=C(N)/C(C#N)=C/C1=CC(C(C)(C)C)=C(O)C(C(C)(C)C)=C1
Synonyms :
AG 879
MDL No. :MFCD00236450
InChI Key :XRZYELWZLNAXGE-KPKJPENVSA-N
Pubchem ID :135419190

Safety of Tyrphostin AG 879

GHS Pictogram:
Signal Word:Warning
Hazard Statements:H302
Precautionary Statements:P280-P305+P351+P338

Related Pathways of Tyrphostin AG 879

RTK

Isoform Comparison

Biological Activity

Target
  • HER2

    HER2-Neu, IC50:1.0 μM

In Vitro:

Cell Line
Concentration Treated Time Description References
Human osteosarcoma U2OS cells 50 µg/mL 4 hours Inhibition of antibody secretion Cells. 2023 Jun 16;12(12):1642.
Rat ovarian cells >4 µM 10 days Inhibition of NTRK3 receptor signaling, resulting in oocyte death and a significant reduction in follicle pool size. Reproduction. 2009 Oct;138(4):697-707.
HEK293 cells 5 µM 12 and 24 hours AG879 inhibits ErbB4 kinase activity, reducing the stability of PSD-95 protein J Neurosci. 2011 Jan 5;31(1):15-25.
A549 cells 10 µM 18 hours Test the inhibitory effect of AG879 on different influenza virus strains, results showed AG879 significantly reduced virus yield. J Virol. 2011 Mar;85(6):2818-27.
SK-BR-3 cells 0.4-20 µM 24-46 hours AG 879 significantly inhibited the proliferation of SK-BR-3 cells by inhibiting the expression of RAF-1 and HER-2, thereby inhibiting the activation of the MAPK signaling pathway. Cell Mol Life Sci. 2004 Oct;61(19-20):2624-31.
MDA-MB-231 cells 0.4-20 µM 24-46 hours AG 879 significantly inhibited the proliferation of MDA-MB-231 cells by inhibiting the expression of RAF-1 and HER-2, thereby inhibiting the activation of the MAPK signaling pathway. Cell Mol Life Sci. 2004 Oct;61(19-20):2624-31.
MCF-7 cells 0.4-20 µM 24-46 hours AG 879 significantly inhibited the proliferation of MCF-7 cells by inhibiting the expression of RAF-1 and HER-2, thereby inhibiting the activation of the MAPK signaling pathway. Cell Mol Life Sci. 2004 Oct;61(19-20):2624-31.
Rat cortical neurons 10 µM 30 min Inhibited Trk receptors, blocking H C-TeTx-induced phosphorylation of Akt, MEK-1/2, ERK-1/2, and p90Rsk Biochem J. 2003 Jul 15;373(Pt 2):613-20.
Rat sensory neurons 30 µM 30 minutes To investigate the effect of AG879 on BDNF-induced sensitization of sensory neurons, results showed that pretreatment with AG879 did not affect the sensitizing action of BDNF. J Physiol. 2008 Jul 1;586(13):3113-27.
GABAergic interneurons 5 µM 4 hours AG879 inhibits ErbB4 kinase activity, leading to increased PSD-95 protein degradation and reduced number and size of PSD-95 puncta J Neurosci. 2011 Jan 5;31(1):15-25.
MDCK cells 10 µM 48 hours Evaluate the effect of AG879 on influenza virus replication, results showed AG879 significantly inhibited viral gene expression and virus yield. J Virol. 2011 Mar;85(6):2818-27.
CHO-K1 cells 3, 10, 20 µM 5-7 minutes Investigated the effect of AG879 on Kv4.2/KChIP2 channels, found AG879 significantly accelerated the inactivation rate and showed use-dependent block. Br J Pharmacol. 2015 Jul;172(13):3370-82.
Hippocampal neurons 20 µM Studied the effect of AG879 on A-type potassium currents in hippocampal neurons, found AG879 significantly inhibited A-type potassium currents. Br J Pharmacol. 2015 Jul;172(13):3370-82.

In Vivo:

Species
Animal Model
Administration Dosage Frequency Description References
Rat Neonatal rats Subcutaneous injection 7.6 mg/kg/day (5-day old rats) and 6.7 mg/kg/day (25-day old rats) Once daily for 5 days Inhibition of NTRK3 receptor signaling in vivo, no significant changes in follicle development rates or oocyte death were observed. Reproduction. 2009 Oct;138(4):697-707.
BALB/c mice Influenza A/PR8 virus infection model Intraperitoneal injection 5 mg/kg Once daily for 5 days Evaluate the antiviral activity of AG879 in a mouse model of influenza virus infection, results showed significant reduction in viral replication and mortality Antimicrob Agents Chemother. 2011 Dec;55(12):5553-9

Protocol

Bio Calculators
Preparing Stock Solutions 1mg 5mg 10mg

1 mM

5 mM

10 mM

3.16mL

0.63mL

0.32mL

15.80mL

3.16mL

1.58mL

31.60mL

6.32mL

3.16mL

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