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A83B4C63

Chemical Structure : A83B4C63

CAS No.: 2245002-14-4

A83B4C63 (PNKP inhibitor)

Catalog No.: PC-73255Not For Human Use, Lab Use Only.

A83B4C63 is a potent small molecule DNA repair protein, polynucleotide kinase 3′-phosphatase (PNKP) inhibitor with Kd of 80 nM.

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

    Biological Activity

    A83B4C63 is a potent small molecule DNA repair protein, polynucleotide kinase 3'-phosphatase (PNKP) inhibitor with Kd of 80 nM.
    A83B4C63 is a nano-encapsulated potent, but poorly water-soluble lead PNKP inhibitor with therapeutic potential for PTEN-deficient CRC.
    Nano-carriers of A83B4C63 effectively inhibited the growth of HCT116/PTEN-/- xenografts in NIH-III nude mice following intravenous (IV) administration, but not that of wild-type HCT116/PTEN+/+ xenografts.
    A83B4C63 encapsulated in NPs (NP/A83) based on mPEO-b-PBCL or solubilized with CE/A83, sensitized colorectal cancer cells to DNA damaging therapeutics in human HCT116 colorectal cancer (CRC) models.

    Physicochemical Properties

    M.Wt 564.598
    Formula C32H28N4O6
    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-(hydroxy(2-methoxyphenyl)methyl)-6-(naphthalen-1-ylmethyl)-1-((4-nitrophenyl)amino)-1,2,4a,7a-tetrahydro-5H-pyrrolo[3,4-b]pyridine-5,7(6H)-dione

    References

    1. Shire Z, et al. Mol Pharm. 2018 Jun 4;15(6):2316-2326.

    2. Sadat SMA, et al. J Control Release. 2021 Jun 10;334:335-352.

    3. Sadat SMA, et al. Front Oncol. 2021 Dec 23;11:772920.

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