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APTO-253 hydrochloride

Chemical Structure : APTO-253 hydrochloride

CAS No.: 1422731-37-0

APTO-253 hydrochloride (APTO253;LOR253;LOR-253)

Catalog No.: PC-35076Not For Human Use, Lab Use Only.

APTO-253 is a small molecule inducer of KLF4, stabilizes G-quadruplex DNA and reduces MYC mRNA expression and protein levels.

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

    Biological Activity

    APTO-253 (LOR-253) hydrochloride is a small molecule inducer of KLF4, stabilizes G-quadruplex DNA and reduces MYC mRNA expression and protein levels.
    APTO-253 is converted intracellularly from a monomer to a ferrous complex [Fe(253)3].
    APTO-253 selectively induces CDKN1A (p21), promotes G0-G1 cell-cycle arrest, and triggers apoptosis in acute myeloid leukemia (AML) cells without producing myelosuppression in various animal species and humans, induces DNA Damage in AML cells.

    Physicochemical Properties

    M.Wt 403.845
    Formula C22H15ClFN5
    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

    2-(6-fluoro-2-methyl-1H-indol-3-yl)-1H-imidazo[4,5-f][1,10]phenanthroline hydrochloride

    References

    1. Tsai CY, et al. Mol Cancer Ther. 2018 Apr 6. doi: 10.1158/1535-7163.MCT-17-0834.

    2. Cercek A, et al. Invest New Drugs. 2015 Oct;33(5):1086-92.

    3. Wang B, et al. Biochem Biophys Res Commun. 2017 Mar 11;484(3):486-492.

    4. Local A, et al. Mol Cancer Ther. 2018 Apr 6. doi: 10.1158/1535-7163.MCT-17-1209.

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