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Tyrphostin AG 879

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

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.

CAS No. 148741-30-4

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

1 Customer Review

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HER2 Signaling Pathway Map

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.

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. Click to purchase: Tween 80	30 mg/mL

Chemical Information

Molecular Weight	316.46
Formula	C₁₈H₂₄N₂OS
CAS No.	148741-30-4
Storage	3 years	-20°C	powder
Storage	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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In vivo Formulation Calculator (Clear solution)

Step 1: Enter information below (Recommended: An additional animal making an allowance for loss during the experiment)

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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.

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

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