Tyrphostin AG 879
Catalog No.S2816 Synonyms: AG 879
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.
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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.
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Choose Selective HER2 Inhibitors
|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.|
AG879 inhibits growth of FET6αS26X cells in a concentration-dependent manner.  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.  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.  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). 
|In vivo||AG879(2 mg) induces a decrease in cancer growth in athymic NOD/SCID mice grafted with HTB-114 or HL-60.  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. |
-  Zhou Y, et al. Cancer Res, 2005, 65(13), 5848-5856.
-  He H, et al. Cancer Biol Ther, 2004, 3(1), 96-101.
-  Larsson LI, et al. Cell Mol Life Sci, 2004, 61(19-20), 2624-2631.
|In vitro||DMSO||36 mg/mL (113.75 mM)|
|Ethanol||3 mg/mL (9.47 mM)|
|In vivo||Add solvents individually and in order:
1% DMSO+30% polyethylene glycol+1% Tween 80
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