ALK degrader 2
ALK degrader 2 is an orally active ALK degrader that degrades EML4-ALK levels (DC50 = 8 nM) and nucleophosmin (NPM) -ALK protein levels (DC50 = 102 nM) . ALK degrader 2 mediates ALK degradation via the Hsp70 chaperone system and ubiquitin-proteasome pathway. ALK degrader 2 induces significant S-phase cell cycle arrest and apoptosis in H3122 cells. ALK degrader 2 shows anti-tumor activity in mice bearing H3122 xenografts. ALK degrader 2 can be used for the study of non-small cell lung cancer (NSCLC) . (Pink: ALK ligand (HY-W754809), Blue: Hyt (HY-W013021), Black: Linker (HY-Y1760), ALK ligand-linker conjugate (HY-175528) ) [1].
Product Specifications
UNSPSC
12352005
Target
Anaplastic lymphoma kinase (ALK) ; Apoptosis; PROTACs
Related Pathways
Apoptosis; PROTAC; Protein Tyrosine Kinase/RTK
Applications
Cancer-Kinase/protease
Field of Research
Cancer
Smiles
O=C(CN1CCN(CC1)C2CCN(CC2)C3=C(C=C4C(C(C)(C5=C(C4=O)C(C=CC(C#N)=C6)=C6N5)C)=C3)CC)NCC7C8CC(C7)C=C8
Molecular Formula
C40H48N6O2
Molecular Weight
644.85
References & Citations
Shipping Conditions
Room temperature
Scientific Category
Reference compound1
Clinical Information
No Development Reported
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