Home Protein Tyrosine Kinase HER2 inhibitor Tyrphostin AG 879

Tyrphostin AG 879

Catalog No.S2816 Synonyms: AG 879

For research use only.

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

Tyrphostin AG 879 Chemical Structure

CAS No. 148741-30-4

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

1 Customer Review

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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 (from reference)

Cell Research:

[3]
  • 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.
Animal Research:

[5]
  • 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.

Solubility (25°C)

In vitro

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

Chemical Information

Molecular Weight 316.46
Formula

C18H24N2OS
CAS No. 148741-30-4
Storage 3 years -20°C powder
2 years -80°C in solvent
Smiles CC(C)(C)C1=CC(=CC(=C1O)C(C)(C)C)C=C(C#N)C(=S)N

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Method for preparing in vivo formulation: Take μL DMSO master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O, mix and clarify.

Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.

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Tech Support

Answers to questions you may have can be found in the inhibitor handling instructions. Topics include how to prepare stock solutions, how to store inhibitors, and issues that need special attention for cell-based assays and animal experiments.

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