TAS 0728

TAS 0728

CAT N°: 33528
Price:

From 129.00 109.65

TAS 0728 is a covalent HER2 inhibitor (IC50 = 36 nM).{57578} It is selective for HER2 over panels of 386 and 374 additional kinases, as well as a panel of 68 non-kinase enzymes, when used at a concentration of 1 µM. TAS 0728 inhibits HER2 autophosphorylation in HER2-overexpressing SK-BR-3 cells but not autophosphorylation of EGFR in EGFR-overexpressing A431 cells. It inhibits the growth of six HER2-amplified breast, lung, and gastric cancer cell lines (GI50s = 1.6-31 nM). TAS 0278 (30 and 60 mg/kg) reduces tumor volume in NCI N87 and BT474 mouse xenograft models.

Territorial Availability: Available through Bertin Technologies only in France

  • Synonyms
    • 4-amino-N-[4-[2-(dimethylamino)-2-oxoethyl]-2,3-dimethylphenyl]-1-[(3R)-1-(1-oxo-2-propen-1-yl)-3-piperidinyl]-1H-pyrazolo[3,4-d]pyrimidine-3-carboxamide
  • Correlated keywords
    • TAS0728 HER-2 nonkinase SKBR BR3 SKBR3 A-431 NCIN87 BT-474
  • Product Overview:
    TAS 0728 is a covalent HER2 inhibitor (IC50 = 36 nM).{57578} It is selective for HER2 over panels of 386 and 374 additional kinases, as well as a panel of 68 non-kinase enzymes, when used at a concentration of 1 µM. TAS 0728 inhibits HER2 autophosphorylation in HER2-overexpressing SK-BR-3 cells but not autophosphorylation of EGFR in EGFR-overexpressing A431 cells. It inhibits the growth of six HER2-amplified breast, lung, and gastric cancer cell lines (GI50s = 1.6-31 nM). TAS 0278 (30 and 60 mg/kg) reduces tumor volume in NCI N87 and BT474 mouse xenograft models.

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