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

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

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 2 years-80°C 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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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 μL 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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HER2 Signaling Pathway Map

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Features:A potent EGFR tyrosine kinase inhibitor.

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Tyrphostin AG 879