Tyrphostin AG 879

Name: Tyrphostin AG 879
Brand: Selleck Chemicals
SKU: S2816
Rating: 5 (2 reviews)

For research use only.

Catalog No.S2816 Synonyms: AG 879

2 publications

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.

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

Br J Pharmacol, 2015, 10.1111/bph.13127

PubMed: ( click the link to review the publication )

Br J Pharmacol, 2015, 172(13):3370-82

PubMed: 25752739 ( click the link to review the publication )

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

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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

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)

References

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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 Download Tyrphostin AG 879 SDF

Molecular Weight	316.46
Formula	C₁₈H₂₄N₂OS
CAS No.	148741-30-4
Storage	3 years -20°C powder
Storage	2 years -80°C in solvent
Synonyms	AG 879
Smiles	CC(C)(C)C1=C(O)C(=CC(=C1)/C=C(C#N)/C(N)=S)C(C)(C)C

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Method for preparing DMSO master liquid: ： mg drug pre-dissolved in μL DMSO (Master liquid concentration mg/mL， Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug. )

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

Note：1.Please make sure the liquid is clear before adding the next solvent.
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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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Features:A potent EGFR tyrosine kinase inhibitor.

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Tyrphostin AG 879