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 (Sturcture Note:(Blue: Cereblon ligand (HY-103596), Black: linker；Pink: ALK/c-Met inhibitor Crizotinib (HY-50878)).

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-med iatedprotein PROTAC-type MET degrader. OZD-MET 01 can inhibit proliferation of H596 and H1437 cells with IC₅₀ values of 3.07 and 3.5 μM. OZD-MET 01 can be used for the research of cancer, such as non-small cell lung cancer. (Structure Note: Pink: MET ligand (HY-50878); Blue: chaperone ligand (HY-112078); MET ligand-Linker: (HY-176950))

PROTAC c-Met degrader-6 is a potent and orally active c-Met PROTACdegrader. PROTAC c-Met degrader-6 significantly induces the degradation of the c-Met protein with DC₅₀s of 0.52 nM and 0.45 nM in EBC-1 and Hs746T. PROTAC c-Met degrader-6 almost abrogates the migratory and invasion abilities of tumor cells and significantly induces the apoptosis and blocks the cell cycle in the G0/G1 phase. PROTAC c-Met degrader-6 can be used for the study of various cancers such as non-small cell lung cancer and stomach cancer.

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 (Compound H11) is an orally active c-Met degrader (through the ubiquitin proteasome system). c-Met degrader-1 has anti-hepatocellular carcinoma activity (HCC) and inhibits tumor growth in MHCC97H xenografts. c-Met degrader-1 inhibits HCC cell growth, arrests cell cycle, and induces apoptosis. c-Met degrader-1 may overcome resistance to type Ib inhibitors.

PROTAC c-Met degrader-5 (Compound D19) is an orally active c-Met PROTAC degrader with DC₅₀s of 0.42 and 0.32 nM in EBC-1 and Hs746T cells, respectively. PROTAC c-Met degrader-5 significantly induces cell apoptosis, G1 cell cycle arrest, and inhibits cell migration and invasion. PROTAC c-Met degrader-5 has potent antiproliferative and degradation efficacy against c-Met-addicted cancer cells and Tepotinib (HY-14721)-resistant cancer cells. Pink: c-Met ligand (HY-W425461); Blue: CRBN ligase ligand (HY-14658); Black: linker