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    Tyrphostin AG 879
    Tyrphostin AG 879

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    This product is for research use only, not for human use. We do not sell to patients.
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    InvivoChem Cat #: V0582
    CAS #: 148741-30-4Purity ≥98%

    Description: Tyrphostin AG 879 (AG-879), a tyrphostin compound, is novel multi-tyrosine kinase inhibitor with potential antitumor activity. It potently inhibits HER2/ErbB2 with an IC50 of 1 μM, shows 100- and 500-fold higher selectivity against ErbB2 over PDGFR and EGFR.  

    ReferencesCancer Res. 2005 Jul 1;65(13):5848-56; Anticancer Drugs. 2006 Sep;17(8):929-41.

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    Molecular Weight (MW)316.46
    FormulaC18H24N2OS
    CAS No.148741-30-4
    Storage-20℃ for 3 years in powder form
    -80℃ for 2 years in solvent
    Solubility (In vitro)DMSO: 36 mg/mL (113.7 mM)
    Water: <1 mg/mL
    Ethanol: 3 mg/mL (9.5 mM)
    Solubility (In vivo)1% DMSO+30% polyethylene glycol+1% Tween 80: 30 mg/mL
    SynonymsAG 879; Tyrphostin AG 879; Tyrphostin AG879; Tyrphostin AG-879; AG879; AG-879; 

    Chemical Name: 2-Propenethioamide, 3-(3,5-bis(1,1-dimethylethyl)-4-hydroxyphenyl)-2-cyano-, (E)-

    InChi Key: XRZYELWZLNAXGE-KPKJPENVSA-N

    InChi Code: InChI=1S/C18H24N2OS/c1-17(2,3)13-8-11(7-12(10-19)16(20)22)9-14(15(13)21)18(4,5)6/h7-9,21H,1-6H3,(H2,20,22)/b12-7+

    SMILES Code: S=C(N)/C(C#N)=C/C1=CC(C(C)(C)C)=C(O)C(C(C)(C)C)=C1


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    In Vitro

    In vitro activity: 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).


    Kinase Assay: TyrphostinAG879 is a tyrosine kinase inhibitor that inhibits TrKA phosphorylation, but not TrKB and TrKC. It is also a ErbB2 kinase inhibitor, has at least 500-fold higher selectivity to ErbB2 (IC50 = 1 μmol/L) than EGFR (IC50 >500 μmol/L).


    Cell Assay: MCF-7 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.

    In VivoAG879(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.
    Animal modelNude mice bearing v-Ha-RAS transformed NIH 3T3 cells
    Formulation & DosageDissolved in 30% DMSO with PBS; 20 mg/kg; i.p. injection
    References

    Cancer Res. 2005 Jul 1;65(13):5848-56; Anticancer Drugs. 2006 Sep;17(8):929-41.


    These protocols are for reference only. InvivoChem does not independently validate these methods.

    Tyrphostin AG 879

    Effect of AG1478 + AG879 on PARP cleavage. Subconfluent FET6αS26X cells were incubated in SM medium with either 5, 10, or 15 μmol/L AG1478 alone or in combination with 1 μmol/L AG879 for 24 hours. Cell lysates were harvested and PARP cleavage was detected using a monoclonal PARP antibody. AG879 concentrations of 5 and 10 μmol/L were used as controls. Cancer Res. 2005 Jul 1;65(13):5848-56.

    Tyrphostin AG 879

    Annexin V and PI double staining for apoptosis. Cancer Res. 2005 Jul 1;65(13):5848-56.

    Tyrphostin AG 879

    Effect of AG1478 + AG879 on inhibition of EGFR and ErbB2 phosphorylation.


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