Chemical Structure : TAS2940
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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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.
M.Wt | 482.588 | |
Formula | C28H30N6O2 | |
Appearance | Solid | |
Storage |
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Solubility |
10 mM in DMSO |
1. Kei Oguchi, et al. Cancer Sci. 2022 Oct 25. doi: 10.1111/cas.15617.
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