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PI3Kα-IN-5

Chemical Structure : PI3Kα-IN-5

CAS No.: 2101744-13-0

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PI3Kα-IN-5 (PI3Kα inhibitor)

Catalog No.: PC-62838Not For Human Use, Lab Use Only.

PI3Kα-IN-5 is a potent, selective PI3Kα inhibitor with enzyme IC50 and cell IC50 of 6 nM and 87 nM respectively, exhibits 100-fold selectivity over PI3Kβ.

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

    Biological Activity

    PI3Kα-IN-5 is a potent, selective PI3Kα inhibitor with enzyme IC50 and cell IC50 of 6 nM and 87 nM respectively, exhibits 100-fold selectivity over PI3Kβ.
    PI3Kα-IN-5 displays high potency and selectivity, and suitable physiochemical and pharmacokinetic properties for oral administration.
    PI3Kα-IN-5 shows good inhibition of tumour growth (86% tumour growth inhibition at 50 mg/kg twice daily orally) in the MCF7 xenograft model in mice.

    Physicochemical Properties

    M.Wt 363.385
    Formula C17H17N9O
    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

    5-(3-amino-6-(imidazo[1,2-a]pyridin-3-yl)-5-methylpyrazin-2-yl)-N,1-dimethyl-1H-1,2,4-triazole-3-carboxamide

    References

    1. Barlaam B, et al. Bioorg Med Chem Lett. 2017 Jul 1;27(13):3030-3035.

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