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Tucatinib
Tucatinib (Irbinitinib, ARRY-380, ONT-380) is an orally available, potent and selective reversible HER2 kinase inhibitor. In both biochemical and cell signaling experiments, tucatinib inhibits HER2 kinase activity with single-digit nanomolar potency (IC50 = 8 nM) and provides exceptional selectivity for HER2 compared with the related EGFR, with a >1,000-fold enhancement in potency for HER2 in cell signaling assays. Tucatinib potently inhibits signal transduction downstream of HER2 and HER3 through the MAPK and PI3K/AKT pathways and is selectively cytotoxic in HER2-amplified breast cancer cell lines in vitro. in vivo, tucatinib is active in multiple HER2+ tumor models as a single agent and shows enhanced antitumor activity in combination with trastuzumab or docetaxel, resulting in improved rates of partial and complete tumor regression (Ref 1).
Catalog NO: CT-TUCA
Synonym: ARRY-380, Irbinitinib, ONT-380
CAS NO: 937263-43-9
Mol. Formula: C26H24N8O2
MW: 480.5
** in vivo Quality Material, >99% pure by HPLC. Hydrate, validated by a spot-on quantitative Elemental Analysis. Bulk stock, prompt.
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