PROTAC RET Degrader 1
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 ; Blue: CRBN ligand (HY-179307) ; Black: Linker).
Product Specifications
CAS Number
2760847-82-1
UNSPSC
12352005
Target
PROTACs; RET
Related Pathways
PROTAC; Protein Tyrosine Kinase/RTK
Applications
Cancer-Kinase/protease
Field of Research
Cancer
Smiles
CCC1(CCN(CC1)C2=NC=C(C=C2)C3=NC(C4=CN(N=C4)[C@H]5CC[C@@H](CC5)N6CCC(CC6)C7=C(C=C(C=C7)NC8CCC(NC8=O)=O)F)=CN9N=CC(C#N)=C39)C(NC(C)C)=O
Molecular Formula
C48H57FN12O3
Molecular Weight
869.04
References & Citations
[1]Orsi DL, et al. Discovery of an orally bioavailable, CNS active pan-mutant RET kinase heterobifunctional degrader. RSC Med Chem. 2025 Aug 13.
Shipping Conditions
Room temperature
Scientific Category
Reference compound1
Clinical Information
No Development Reported
Isoform
Cereblon
Frequently Asked Questions
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