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Tyrphostin AG 879

Catalog No. T6712 CAS 148741-30-4

Synonyms: AG 879

Tyrphostin AG 879 effectively inhibits HER2/ErbB2 (IC50: 1 μM), 100- and 500-fold higher selective to ErbB2 than EGFR and PDGFR.

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Tyrphostin AG 879, CAS 148741-30-4

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Purity: 98%

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Description	Tyrphostin AG 879 effectively inhibits HER2/ErbB2 (IC50: 1 μM), 100- and 500-fold higher selective to ErbB2 than EGFR and PDGFR.
Targets&IC50	HER2/ErbB2:1 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]
Kinase Assay	AZD3759 is tested at a single 1 μM concentration across each of 124 kinases from Millipore kinase panel at an ATP concentration that is within 15 μM of their corresponding apparent Km values. In brief, recombinant kinases are incubated within an appropriate buffer containing peptide substrate and radiolabelled γ-33P-ATP together with presence or absence of required inhibitor concentration. The reaction is initiated by adding ATP/Mg2+ mix. After incubation for 40 minutes at room temperature, the reaction is stopped by adding 3% phosphoric acid solution. A portion of reaction mix is spotted onto P30 filter mat to trap peptide and washed three times for 5 minutes with phosphoric acid to remove non-specific γ-33P-ATP. The phosphorylated substrate is then measured by scintillation counting, which determined the level of kinase activity inhibition compared to control reactions[1].
Cell Research	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)

Synonyms	AG 879
Molecular Weight	316.46
Formula	C18H24N2OS
CAS No.	148741-30-4

Storage

Powder: -20°C for 3 years

In solvent: -80°C for 2 years

Solubility Information

DMSO: 31.7 mg/mL (100 mM)

Ethanol: 7.9 mg/mL (25 mM)

( < 1 mg/ml refers to the product slightly soluble or insoluble )

References and Literature

1. Zhou Y, et al. Cancer Res, 2005, 65(13), 5848-5856. 2. He H, et al. Cancer Biol Ther, 2004, 3(1), 96-101. 3. Larsson LI, et al. Cell Mol Life Sci, 2004, 61(19-20), 2624-2631. 4. Rende M, et al. Anticancer Drugs, 2006, 17(8), 929-941. 5. He H, et al. Cancer J, 2001, 7(3), 191-202. 6. Zhou Y et al. Blockade of EGFR and ErbB2 by the novel dual EGFR and ErbB2 tyrosine kinase inhibitor GW572016 sensitizes human colon carcinoma GEO cells to apoptosis. Cancer Res. 2006 Jan 1;66(1):404-11.

Related compound libraries

This product is contained In the following compound libraries：

Anti-Cancer Compound Library Anti-Lung Cancer Compound Library Anti-Pancreatic Cancer Compound Library Inhibitor Library Immuno-Oncology Compound Library Immunology/Inflammation Compound Library Anti-Breast Cancer Compound Library Kinase Inhibitor Library Apoptosis Compound Library Epigenetics Compound Library

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Keywords

Tyrphostin AG 879 148741-30-4 JAK/STAT信号通路蛋白酪氨酸激酶凋亡血管生成 Apoptosis EGFR HER PDGFR Trk receptor tyrosine phosphorylation Tyrphostin AG-879 antiproliferation Tyrphostin AG879 ErbB2 Trk Receptor ErbB-1 TrKA Antitumor Tropomyosin related kinase receptor Inhibitor AG-879 p75 Epidermal growth factor receptor HER1 inhibit AG 879 AG879 inhibitor

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