QZ2135

QZ2135 (compound 20) is a RET-targeted PROTAC degrader with in vivo antitumor properties in a Ba/F3-KIF5B-RET-G810C xenograft mouse model. The degradation activities of QZ2135 targeting KIF5B-RET have DC50 values of 4.7 nM (WT), 17.2 nM (V804M), and 73.8 nM (G810C), respectively. QZ2135 is composed of a target protein ligand (red part) RET ligand-3 (HY-170853), an E3 ligase ligand (blue part) Lenalidomide-F (HY-W039233), and a PROTAC Linker (black part) 7-Iodohept-1-yne (HY-W587352), in which the target protein ligand + linker form a conjugate RET Ligand-Linker Conjugate-1 (HY-170854) [1].

Product Specifications

UNSPSC

12352005

Target

PROTACs; RET

Related Pathways

PROTAC; Protein Tyrosine Kinase/RTK

Applications

Cancer-Kinase/protease

Field of Research

Cancer

Smiles

N#CC1=C2C(C3=CC=C(N4CC(C5)N(CC6=CC=C(OC)N=C6)C5C4)N=C3)=CC(C7=CN(C8CCN(CCCCCC#CC9=CC=CC%10=C9CN(C(CC%11)C(NC%11=O)=O)C%10=O)CC8)N=C7)=CN2N=C1

Molecular Formula

C53H54N12O4

Molecular Weight

923.07

References & Citations

[1]Zhang Q, et al. Discovery of an Efficacious RET PROTAC Degrader with Enhanced Antiproliferative Activity against Resistant Cancer Cells Harboring RET Solvent-Front Mutations. J Med Chem. 2025 Jan 9;68 (1) :753-775.