c-Met/HGFR Degrader

PRO-6E is an oral active PROTAC based on Cereblon ligand, and induces the degradation of MET with maximum degradation of 81.9% at 1 μM in MKN-45 cells. PRO-6E inhibits tumor growth in vivo and in vitro. PRO-6E induces cell apoptosis and induces cell arrest.

SJF-8240 is a selective p38α and c-Met PROTAC degrader. SJF-8240 promotes the ubiquitination and selective degradation of p38α and c-Met. SJF-8240 is applicable to breast cancer-related research.

PROTAC c-Met degrader-1 is a selective and orally active c-Met PROTAC degrader with a DC₅₀ of 6.21 nM against c-Met. PROTAC c-Met degrader-1 induces CRBN-dependent ubiquitination and proteasomal degradation of c-Met. PROTAC c-Met degrader-1 induces G0/G1 phase arrest in c-Met-dependent cancer cells. PROTAC c-Met degrader-1 kills c-Met-dependent cancer cells. PROTAC c-Met degrader-1 inhibits tumor growth in animal models. PROTAC c-Met degrader-1 can be used for the research of gastric cancer.

PROTAC c-Met degrader-3 is a c-Met PROTAC degrader with a DC₅₀ of 0.59 nM. PROTAC c-Met degrader-3 induces ubiquitination and degradation of c-Met. PROTAC c-Met degrader-3 induces Apoptosis. PROTAC c-Met degrader-3 can be used in lung cancer-related research.

OZD-MET 01 is a chaperone-based PROTAC-class MET protein degrader. OZD-MET 01 induces MET protein degradation in lung cancer cells in a time- and dose-dependent manner and inhibits cancer cell proliferation. OZD-MET 01 can be used in studies related to non-small cell lung cancer.

PROTAC c-Met degrader-6 is an orally active c-Met PROTAC degrader with DC₅₀ values of 0.52 nM (EBC-1) and 0.45 nM (Hs746T), respectively. PROTAC c-Met degrader-6 induces potent targeted degradation of c-Met via the ubiquitin-proteasome system by bridging the target protein c-Met and the Cullin-CRBN E3 ubiquitin ligase to form a ternary complex, thereby inducing tumor cell cycle arrest and apoptosis. PROTAC c-Met degrader-6 can be used in the research of various MET-driven cancers (such as gastric cancer, liver cancer, non-small cell lung cancer, etc.).

VERT-002 is a MET degrader and monoclonal antibody. VERT-002 induces nearly complete and profound degradation of the MET protein by enhancing the intrinsic shedding of the MET extracellular domain (ECD). VERT-002 demonstrates significant anti-tumor activity. VERT-002 can be used in non-small cell lung cancer research..

PROTAC c-Met Degrader-4 (compound D15) is a potent orally active PROTAC c-MET degrader. PROTAC c-Met Degrader-4 demonstrates excellent intracellular degradation potency with a DC₅₀ < 0.5 nM. PROTAC c-Met Degrader-4 induces cell cycle arrest and apoptosis, inhibits cell invasion and migration, thereby suppressing cell proliferation. PROTAC c-Met Degrader-4 inhibits the growth of Hs746T xenograft tumors in nude mice. PROTAC c-Met Degrader-4 can be used for cancer research, such as non-small cell lung cancer and gastric cancer.

PROTAC c-Met degrader-2 (PROTAC2) is a PROTAC-based c-Met degrader, with a DC₅₀ of 50 nM.

c-Met degrader-1 is an orally active c-Met HyT degrader with a DC₅₀ of 226.12 nM. c-Met degrader-1 exhibits anticancer activity against hepatocellular carcinoma. c-Met degrader-1 can be used in the research of hepatocellular carcinoma (HCC) (c-Met ligand: Tepotinib (HY-14721), hydrophobic tag moiety: Adamantan-1-ylmethanamine (HY-W037848)).

PROTAC c-Met degrader-5 is an orally active c-Met PROTAC degrader. PROTAC c-Met degrader-5 induces c-Met degradation via Cullin-CRBN, with a DC₅₀ value of 0.32 nM, and inhibits the phosphorylation of c-Met and its downstream signaling molecule STAT3. PROTAC c-Met degrader-5 inhibits cancer cell proliferation, migration and invasion, induces apoptosis, alters cell cycle distribution, and suppresses the growth of EBC-1 xenograft tumors. PROTAC c-Met degrader-5 can be used to study MET-driven cancers as well as Tepotinib (HY-14721)-resistant cancers harboring c-Met^D1228N and c-Met^Y1230H mutations.