Tyrphostin AG 879

Catalog No.S2816 Batch:S281601

Technical Data

Formula

C₁₈H₂₄N₂OS

Molecular Weight

316.46

CAS No.

148741-30-4

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)

Clear solution

5%DMSO 1 40%PEG300 2 5%Tween80 3 50%ddH2O

1.5mg/ml

Taking the 1 mL working solution as an example, add 50 μL of 30 mg/ml clarified DMSO stock solution to 400 μL of PEG300, mix evenly to clarify it; add 50 μL of Tween80 to the above system, mix evenly to clarify; then continue to add 500 μL of ddH2O to adjust the volume to 1 mL. The mixed solution should be used immediately for optimal results.

* <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.
* Room temperature shipping (Stability testing shows this product can be shipped without any cooling measures.)

Preparing Stock Solutions

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 Assay:^{^[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 Study:^{^[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.

Cell Assay:^{^[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 Study:^{^[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.

References

+ Expand

Customer Product Validation

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

Selleck's Tyrphostin AG 879 has been cited by 3 publications

The molecular and functional landscape of resistance to immune checkpoint blockade in melanoma [ Nat Commun, 2023, 14(1):1516]	PubMed: 36934113
Effect of tyrphostin AG879 on Kv 4.2 and Kv 4.3 potassium channels. [ Br J Pharmacol, 2015, 172(13):3370-82]	PubMed: 25752739
Effect of Tyrphostin AG879 on Kv4.2 and Kv4.3 potassium channels 1 Running title: Tyrphostin AG879 inhibits Kv4.2 and Kv4.3 potassium channels [Yu H, et al. Br J Pharmacol, 2015, 10.1111/bph.13127 ]

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SHIPPING AND STORAGE
Selleck products are transported at room temperature. If you receive the product at room temperature, please rest assured, the Selleck Quality Inspection Department has conducted experiments to verify that the normal temperature placement of one month will not affect the biological activity of powder products. After collecting, please store the product according to the requirements described in the datasheet. Most Selleck products are stable under the recommended conditions.

NOT FOR HUMAN, VETERINARY DIAGNOSTIC OR THERAPEUTIC USE.