Catalog No.: PC-38023Not For Human Use, Lab Use Only.
Tucatinib (Irbinitinib, ONT-380, ARRY-380) is a potent, selective, reversible and ATP-competitive inhibitor of ErbB-2 (HER2) with IC50s of 8 nM and 7 nM for ErbB-2 and p95 HER2, respectively.
Tucatinib (Irbinitinib, ONT-380, ARRY-380) is a potent, selective, reversible and ATP-competitive inhibitor of ErbB-2 (HER2) with IC50s of 8 nM and 7 nM for ErbB-2 and p95 HER2, respectively.
Tucatinib displays 500-fold selective for HER2 versus EGFR in cell-based assays.
Tucatinib inhibits the phosphorylation of HER2 in a L755S mutant MCF-10A cell line and inhibits the growth of 3 L755S mutant tumor models derived from colorectal, gastric and non-small cell lung cancer.
Tucatinib also potently inhibits the phosphorylation of HER2 in a V777L mutant MCF-10A cell line, and in a colorectal PDX model containing a V777L mutation, tucatinib alone or in combination with trastuzumab induces tumor regressions.
Tucatinib inhibits HER2 phosphorylation, but not EGFR phosphorylation, and inhibits the phosphorylation of HER2, HER3, Erk1/2, MEK1 and AKT in the G776V_G/C HER2 mutant NCI-H1781 cell line.
