2. Signaling Pathways
  3. Protein Tyrosine Kinase/RTK
  4. RET
  5. RET Degrader

RET Degrader

RET Degraders (5):

Cat. No. Product Name Effect Purity
  • HY-179308
    RET ligand-5
    		Degrader
    RET ligand-5 is a PROTAC target protein ligand that can be used for synthesis of PROTACs, such as PROTAC RET Degrader 1 (HY-178964). PROTAC RET Degrader 1 is a potent RET PROTAC degrader with anti-tumor activity.
  • HY-170852
    QZ2135
    		Degrader
    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).
  • HY-170855A
    YW-N-7 TFA
    		Degrader
    YW-N-7 (TFA) is a PROTAC that targets both the inhibition and degradation of RET kinase, with a DC50 of 88 nM. YW-N-7 (TFA) exhibits antitumor activity in a KIF5B-RET-driven xenograft mouse tumor model and can be used in the area of cancer (Structure: red part represents the target protein ligand: HY-170856; blue part represents the E3 ligase ligand: HY-1708557; black part represents the linker; E3 ligase ligand + linker: HY-170858).
  • HY-170853
    RET ligand-3
    		Degrader
    RET ligand-3 is the ligand for targeting RET PROTAC QZ2135 (HY-170852).
  • HY-178964
    PROTAC RET Degrader 1
    		Degrader
    PROTAC RET Degrader 1 (Compound 20) is an orally active and blood-brain barrier-crossing RET PROTAC degrader with DC50 values for RET (WT), RET (G810S), RET (G810C), and RET (G810R) of 1.7, 3, 12, and 21 nM, respectively. PROTAC RET Degrader 1 exhibits potent anti-proliferative activity in cancer cell lines carrying oncogenic RET fusions (such as KIF5B-RET, CCDC6-RET) or mutations (such as RET (C634W)). PROTAC RET Degrader 1 shows significant anti-tumor activity in human tumor xenograft (PDX) mouse models. PROTAC RET Degrader 1 can be used for the study of RET-positive cancers Pink: RET ligand (HY-179308); Blue: CRBN ligand (HY-179307); Black: Linker).