Tyrphostin AG 879

Catalog No.S2816 Synonyms: AG 879

Tyrphostin AG 879 Chemical Structure

Molecular Weight(MW): 316.46

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

Size Price Stock Quantity  
In DMSO USD 90 In stock
USD 70 In stock
USD 110 In stock
USD 270 In stock

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1 Customer Review

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

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Notes:

2. For more details, such as half maximal inhibitory concentrations (IC50s) and working concentrations of each inhibitor, please click on the link of the inhibitor of interest.
3. "+" indicates inhibitory effect. Increased inhibition is marked by a higher "+" designation.
4. Orange "√" refers to compounds which do inhibitory effects on the related isoform, but without specific value.

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] Trk [6] PDGFR [6] EGFR [6]
1.0 μM 10 μM >100 μM >500 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
+ Expand
  • 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
+ Expand
  • Animal Models: nude mice carrying v-Ha-RAS transformed NIH 3T3 cells
  • Formulation: 30% dimethyl sulfoxide with PBS
  • 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 <1 mg/mL
In vivo 1% DMSO+30% polyethylene glycol+1% Tween 80 30 mg/mL

* 1 mg/ml means slightly soluble or insoluble.
* 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

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HER2 Signaling Pathway Map

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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID