Medchemexpress LLC Tucatinib hemiethanolate | 1429755-56-5 | 98.8% | 503.57 | 5 MG

Supplier:  Medchemexpress LLC HY16069A5MG

Tucatinib hemiethanolate is a potent, orally active, and selective HER2 inhibitor (IC50: 8 nM) with ~500-fold selectivity over EGFR in cell-based assays. It selectively blocks proliferation and phosphorylation of HER2 and its downstream effector, Akt, in HER2 overexpressing cell lines, offering potential to block HER2 signaling without the toxicities associated with EGFR inhibition.

• Potent, orally active, selective HER2 inhibitor.
• Exhibits ~500-fold selectivity for HER2 over EGFR.
• Blocks HER2 proliferation and Akt phosphorylation.
• May avoid EGFR inhibition toxicities.
• Shows survival benefit and reduces brain pErbB2 in animal models.
• Demonstrates significant dose-related tumor growth inhibition.
• Combined with trastuzumab, shows 98% tumor growth inhibition.

Catalog No. 50-003-91821