Tyrphostin AG 879

For research use only.

Catalog No.S2816 Synonyms: AG 879

2 publications

Tyrphostin AG 879 Chemical Structure

CAS No. 148741-30-4

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

Selleck's Tyrphostin AG 879 has been cited by 2 publications

1 Customer Review

  • Identification of tyrphostin AG879 as a Kv4.2 channel inhibitor. (A) Chemical structure of AG879. (B) Effect of AG879 on Kv4.2 channels in CHO-K1 cells. AG879 10 μM reduced the Kv4.2-mediated peak current by 31.27 ± 2.4%. The Kv4.2 channel currents were recorded by a depolarization to +40 mV for 300 ms from a holding potential −80 mV. (C) Inhibition by AG879 3, 10 and 20 μM of Kv4.2/KChIP2 co-expressed channels. (D) Concentration-dependent inhibition by AG879 of Kv4.2/KChIP2 channel shown by measuring peak and integral currents. Concentration–response curves for AG879 were fitted to the Hill equation. (E) Reversible inhibition of Kv4.2 by AG879. Maximal inhibition occurred ∼5 min after drug application. (F) Concentration-dependent inhibition by AG879 of Kv4.3 channels.

    Br J Pharmacol, 2015, 172(13):3370-82.. Tyrphostin AG 879 purchased from Selleck.

Purity & Quality Control

Choose Selective HER2 Inhibitors

Biological Activity

Description Tyrphostin AG 879 potently inhibits HER2/ErbB2 with IC50 of 1 μM, 100- and 500-fold higher selective to ErbB2 than PDGFR and EGFR.
Targets
HER2-Neu [6]
(Cell-free assay)		 Trk [6]
(Cell-free assay)
1.0 μM 10 μM
In vitro

AG879 inhibits growth of FET6αS26X cells in a concentration-dependent manner. [1] AG879(10 nM) blocks the activation of PAK1 and suppresses RAS-induced malignant transformation of NIH 3T3 cells. AG879(<1 μM) inhibits the Tyr-phosphorylation of ERK and its association with PAK1 in v-Ha-RAS-transformed NIH 3T3 fibroblasts. [2] AG 879 dose-dependently reduce MCF-7 cell numbers and show already a significant effect at 0.4 mM through inhibiting DNA synthesis and mitotic. AG 879(<20 μM) inhibits activation of ERK-1/2 in MCF-7 cell. AG 879(5 μM) decreases expression of Hsp90 client proteins RAF-1 and HER-2. [3] AG879(20 μM) dramatically decreases proliferation with a variable increase in apoptosis in Cell lines from human leiomyosarcoma (HTB-114, HTB-115, HTB-88), rhabdomyosarcoma (HTB-82, TE-671), prostatic adenocarcinoma (PC-3), acute promyelocytic leukemia (HL-60) and histiocytic lymphoma (U-937). [4]
In vivo AG879(2 mg) induces a decrease in cancer growth in athymic NOD/SCID mice grafted with HTB-114 or HL-60. [4] AG 879(20 mg/kg) treatment keeps 50% of mice absolutely free of RAS-induced sarcomas, and dramatically reduces the size of the growing sarcomas in the nude mice carrying v-Ha-RAS transformed NIH 3T3 cells. [5]

Protocol

Cell Research:

[3]
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  • Cell lines: MCF-7 cells
  • Concentrations: 20 μM
  • Incubation Time: 46 hours
  • Method:

    Cells are grown in 96-well plates containing 100 μL medium per well. Ten microliters of MTT solution (5 mg/ml in PBS) is added to each well and incubation continued for 4 h at 37 °C. Subsequently, 100 μL 10% SDS in 0.01 M HCl is added. After incubation at 37°C overnight, absorption is measured at 550 nm in an ELISA reader using a reference filter of 690 nm.


    (Only for Reference)
Animal Research:

[5]
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  • Animal Models: nude mice carrying v-Ha-RAS transformed NIH 3T3 cells
  • Dosages: 20 mg/kg
  • Administration: Intraperitoneally administrated on days 3, 5, 7, 10, 12, 14, and 17.
    (Only for Reference)

Solubility (25°C)

In vitro DMSO 36 mg/mL (113.75 mM)
Ethanol 3 mg/mL (9.47 mM)
Water Insoluble
In vivo Add solvents to the product individually and in order(Data is from Selleck tests instead of citations):
1% DMSO+30% polyethylene glycol+1% Tween 80
For best results, use promptly after mixing. 		30 mg/mL

* Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations.

Chemical Information

Molecular Weight 316.46
Formula

C18H24N2OS
CAS No. 148741-30-4
Storage powder
in solvent
Synonyms AG 879
Smiles CC(C)(C)C1=CC(=CC(=C1O)C(C)(C)C)C=C(C#N)C(=S)N

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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID