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    Tyrphostin 9 (AG17; Malonoben)
    Tyrphostin 9 (AG17; Malonoben)

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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 #: V0564
    CAS #: 10537-47-0Purity ≥98%

    Description: Tyrphostin-9 (also named as Malonoben; SF-6847; RG-50872; AG-17; GCP-5126; NSC-242557) is a novel and potent epidermal growth factor receptor (EGFR) inhibitor with potential anticancer activity. It inhibits EGFR with an IC50 value of 460 µM in the human epidermoid carcinoma cell line A431. It shows potent anti-proliferative activity in vitro against various cancer cell lines such as PDGF-dependent SMC with IC50 value of 40 nM.

    References: J Med Chem. 1989 Oct;32(10):2344-52; Proc Natl Acad Sci U S A. 2008 Aug 12;105(32):11218-23. 

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    Molecular Weight (MW)282.38
    FormulaC18H22N2O
    CAS No.10537-47-0
    Storage-20℃ for 3 years in powder form
    -80℃ for 2 years in solvent
    Solubility (In vitro)DMSO: 56 mg/mL (198.3 mM)
    Water: <1 mg/mL
    Ethanol: 56 mg/mL (198.3 mM)
    Solubility (In vivo)

    Chemical Name: 2-[[3,5-bis(1,1-dimethylethyl)-4-hydroxyphenyl]methylene]-propanedinitrile

    InChi Key: MZOPWQKISXCCTP-UHFFFAOYSA-N

    InChi Code: InChI=1S/C18H22N2O/c1-17(2,3)14-8-12(7-13(10-19)11-20)9-15(16(14)21)18(4,5)6/h7-9,21H,1-6H3

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

    SynonymsRG50872; SF-6847; RG-50872; AG-17; GCP-5126; NSC-242557; SF6847; RG50872; AG17; GCP5126; NSC242557; SF 6847; RG 50872; AG 17; GCP 5126; NSC 242557; Tyrphostin-9; Tyrphostin 9; Tyrphostin9; Malonoben; Tyrphostin AG17; 


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    In Vitro

    In vitro activity: SF 6847 inhibits the replication of herpes simplex virus type 1 (HSV-1) with IC50 of 40 nM. SF 6847 (50 nM) partly reverses sodium orthovanadate induced HSV-1 plaque formation. SF 6847 (< 400 nM) decreases the phosphorylation of viral phosphoproteins in a dose-dependent manner, but the SF 6847 (< 800 nM)-induced reduction of protein synthesis is not dose-dependent. SF 6847 prevents PDGF-induced tyrosine phosphorylation of LRP in caveolae in human fibroblasts suggesting that PDGF-BB-mediated LRP activation requires tyrosine phosphorylation and therefore activation of PDGFR-β. SF 6847 (1 mM) blocks the strain-induced stimulatory effect on DNA synthesis of fetal lung cells. SF 6847 (1 μM) causes increased exon inclusion of MAPT exon 10. SF 6847 does not affect the translation or stability of the two mRNAs. SF 6847 (1.6 μM) increases the inclusion of MAPT exon 10 by 2-fold in SHSY-5Y cells.


    Kinase Assay: Tyrphostin A9, a tyrosine kinase inhibitor, is a potent inducer of mitochondrial fission. Tyrphostin A9 emerged as the most potent and selective of 51 tyrosine kinase inhibitors tested against the TNF-induced respiratory burst. 


    Cell Assay: Tyrphostin A9 inhibited TNF-induced tyrosine phosphorylation of pyk2 without blocking the cells' bactericidal activity. Tyrphostin A9 is a PDGF receptor tyrosine kinase inhibitor (IC50 = 500 nM). Recent findings suggest that signaling via PDGF receptor tyrosine kinases is not necessary for the shift of the smooth muscle cells from a contractile to a synthetic phenotype. On the other hand these enzymes apparently carry out important functions in the control of intracellular membrane traffic and cell division.

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    References

    J Med Chem. 1989 Oct;32(10):2344-52; Proc Natl Acad Sci U S A. 2008 Aug 12;105(32):11218-23. 


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

    Tyrphostin 9

    Effect of digoxin, tyrphostin-9, and 5-iodotubercidin on the splicing of the endogenous MAPT exon 10. Illustrated is RT-PCR showing the splicing of the endogenous MAPT exon 10 in SHSY-5Y cells. Proc Natl Acad Sci U S A. 2008 Aug 12; 105(32): 11218–11223.

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