TAS2940 | pan-ERBB inhibitor | Probechem Biochemicals

Chemical Structure : TAS2940

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TAS2940 (TAS-2940)

货号: 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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生物&药学活性

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.

物理化学性质&存储条件

分子量	482.588
分子式	C28H30N6O2
外观性状	Solid
CAS No.
储存条件	固体粉末 -20°C 12 个月; 4°C 6 个月	配置液 -80°C 6 个月; -20°C 6 个月
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

参考文献

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

TAS2940 (TAS-2940)

生物&药学活性

物理化学性质&存储条件

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TAS2940 (TAS-2940)

生物&药学活性

物理化学性质&存储条件

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