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TAS2940

Chemical Structure : TAS2940

CAS No.: 2451398-65-3

TAS2940 (TAS-2940)

Catalog No.: PC-49395Not For Human Use, Lab Use Only.

TAS2940 (TAS-2940) is a potent, selective, orally active, irreversible and brain-penetrable pan-ERBB inhibitor with IC50 of 5.6 nM、2.1 nM and 1.0 nM for HER2、HER2 V777L and A775_G776insYVMA, respectively.

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    Biological Activity

    TAS2940 (TAS-2940) is a potent, selective, orally active, irreversible and brain-penetrable pan-ERBB inhibitor with IC50 of 5.6 nM、2.1 nM and 1.0 nM for HER2、HER2 V777L and A775_G776insYVMA, respectively.
    TAS2940 selectively inhibits phosphorylation of targets and the growth of cancer cells with ERBB aberrations in vitro.
    TAS2940 is highly potent against cells harboring HER2/EGFR alteration.
    TAS2940 also inhibited tumor growth in xenograft mouse models with ERBB aberrations: HER2 amplification, HER2/EGFR exon 20 insertions, and EGFR vIII mutation.
    TAS2940 was effective in the intracranial xenograft models of HER2/EGFR cancers and improved the survival of mice models.

    Physicochemical Properties

    M.Wt 482.588
    Formula C28H30N6O2
    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

    7-((3R,5S)-1-acryloyl-5-methylpyrrolidin-3-yl)-4-amino-6-(cyclopropylethynyl)-N-((R)-1-phenylethyl)-7H-pyrrolo[2,3-d]pyrimidine-5-carboxamide

    References

    1. Kei Oguchi, et al. Cancer Sci. 2022 Oct 25. doi: 10.1111/cas.15617.

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