ALK degrader 1

ALK degrader 1 is a potent, hydrophobic tag (HyT) -based degrader that induces ubiquitin-proteasome system (UPS) -dependent EML4-ALK degradation (DC50 = 0.13 μM) . ALK degrader 1 demonstrates potent ALK degradation and antiproliferative effects in ALK-dependent cell lines, while showing minimal cytotoxicity in ALK fusion-negative cells. ALK degrader 1 triggers cell cycle arrest at the G0/G1 phase and stimulates apoptosis. ALK degrader 1 not only facilitates efficient degradation of the ALK protein but also disrupts key downstream effectors, including the STAT3 signaling axis. ALK degrader 1 mediates robust EML4-ALK degradation in vivo. ALK degrader 1 can be used for ALK-related diseases research[1].

C39H47N5O2

617.82

O=C(C(C=C(CC)C(N1CCN(CCCC(NC2(C3)C[C@@H](C4)C[C@H]3C[C@@H]4C2)=O)CC1)=C5)=C5C6(C)C)C7=C6NC8=CC(C#N)=CC=C87

Anaplastic lymphoma kinase (ALK) ; Apoptosis; PROTACs; STAT

Room temperature