RET Degrader

QZ2135 is a CRBN-recruiting PROTAC degrader targeting RET kinase, with a DC₅₀ of 4.7 nM. QZ2135 induces RET degradation via the ubiquitin-proteasome system, while blocking RET phosphorylation and downstream signaling pathways, thereby inhibiting the proliferation and inducing apoptosis of cancer cells expressing wild-type or mutant RET. QZ2135 is applicable for cancer research.

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.

ZW-18-116 (compound 9) is a dual-target PROTAC degrader for the oncoproteins TRKA and RET. ZW-18-116 induces the degradation of oncoproteins TRKA and RET by recruiting the CRBN E3 ligase. ZW-18-116 exhibits potent anti-proliferative activity in various cancer cell lines harboring RET or TRKA fusions. ZW-18-116 can be used for RET or TRKA-derived cancer research, such as thyroid, lung, and colon cancers.

YW-N-7 TFA is a PROTAC degrader targeting RET kinase, with an IC₅₀ of 8.4 nM. YW-N-7 TFA inhibits RET kinase activity and induces proteasome-mediated degradation of RET fusion proteins, while enhancing the anti-tumor activity of Selpercatinib (LOXO-292) (HY-114370). YW-N-7 TFA can be used in the research of cancers associated with RET gene abnormalities, including medullary thyroid carcinoma, papillary thyroid carcinoma and non-small cell lung cancer.

ZW-6-052 (compound 20), the derivative of ZW-18-116 (HY-180550), is a dual-target PROTAC degrader for the oncoproteins TRKA and RET. ZW-6-052 induces degradation of TMP3-TRKA in KM12 mouse xenograft models. ZW-6-052 can be used for RET or TRKA-derived cancer research, such as thyroid, lung, and colon cancers.

RET ligand-3 is a ligand targeting RET, which can be used to synthesize the PROTAC QZ2135 (HY-170852). RET ligand-3 inhibits the RET signaling pathway, induces apoptosis in RET-expressing cells, and exhibits in vivo anti-tumor efficacy in xenograft models. RET ligand-3 is applicable for cancer-related research.

PROTAC RET Degrader 2 is a RET degrader with a target IC₅₀ of 0.36 nM. PROTAC RET Degrader 2 is mainly composed of RET-IN-34 (HY-183729) and Thalidomide (HY-14658). PROTAC RET Degrader 2 mediates RET degradation via the ubiquitin-proteasome system. PROTAC RET Degrader 2 induces apoptosis, inhibits colony-forming ability, and exhibits antiproliferative activity in cancer cells. PROTAC RET Degrader 2 suppresses tumor growth in xenograft models. PROTAC RET Degrader 2 can be used in research related to medullary thyroid carcinoma, papillary thyroid carcinoma, and RET fusion-positive lung adenocarcinoma.

PROTAC RET Degrader 1 is an orally active, blood-brain barrier-penetrant RET PROTAC degrader with a DC₅₀ of 1.7 nM. PROTAC RET Degrader 1 binds to CRBN and forms a ternary complex with RET, mediating proteasomal degradation of RET, while also selectively mediating the degradation of SALL4. PROTAC RET Degrader 1 inhibits the RET signaling pathway, hERG channel activity, and Cyp3A4 enzyme activity; it suppresses cancer cell growth and induces tumor regression. PROTAC RET Degrader 1 can be used in research related to RET-driven cancers.

RET degrader-1 is a HyT degrader targeting RET. RET degrader-1 induces the degradation of CCDC6-RET via the ubiquitin-proteasome pathway. RET degrader-1 can be used in the research of RET-driven cancers.

RD-23 is an orally active and selective RET PROTAC degrader, with DC₅₀ values of 5.6 nM and 11.7 nM against RET^WT and RET^G810C mutants, respectively. RD-23 inhibits purified RET kinase activity with an IC₅₀ of 0.371 nM. RD-23 suppresses the activation of downstream Shc signaling and induces apoptosis. RD-23 can be used for the research of RET-related cancers.