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A-800141

Chemical Structure : A-800141

CAS No.: 681245-85-2

A-800141 (A800141)

Catalog No.: PC-63347Not For Human Use, Lab Use Only.

A-800141 is a potent, highly specific, orally bioavailable MetAP2 inhibitor with IC50 of 12 nM, shows no inhibition for MetAP1 (IC50>30 uM).

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Purity & Documentation Purity: >98% (HPLC) Select Batch:

    Biological Activity

    A-800141 is a potent, highly specific, orally bioavailable MetAP2 inhibitor with IC50 of 12 nM, shows no inhibition for MetAP1 (IC50>30 uM).
    A-800141 also shows a greater selectivity against other aminopeptidases, as well as a CEREP panel of >80 receptors.
    A-800141 causes the formation of GAPDH variants with an unprocessed N-terminal methionine in cell cultures in vitro.
    A-800141 exhibits an antiangiogenesis effect and a broad anticancer activity in a variety of tumor xenografts including B cell lymphoma, neuroblastoma, and prostate and colon carcinomas, either as a single agent or in combination with cytotoxic agents.
    A-800141 blocks tumor growth and MetAP2 activity in mouse models, which are causally connected to MetAP2 inhibition in vivo.

    Physicochemical Properties

    M.Wt 442.574
    Formula C24H30N2O4S
    Appearance Solid
    CAS No.
    Storage
    Solide Powder
    -20 °C 12 Months; 4°C 6 Months
    In Solvent
    -80 °C 6 Months; -20°C 6 Months
    Shipping
    Solubility

    10 mM in DMSO

    Chemical Name/SMILES

    (Z)-2-((2-(3-(diethylamino)prop-1-en-1-yl)phenyl)sulfonamido)-5,6,7,8-tetrahydronaphthalene-1-carboxylic acid

    References

    1. Wang J, et al. Proc Natl Acad Sci U S A. 2008 Feb 12;105(6):1838-43.

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