VEGFR Degrader

VEGFR-2-IN-39 (PROTAC-5) is a PROTAC targeting VEGFR-2 (IC₅₀: 208.6 nM). VEGFR-2-IN-39 has low toxicity.VEGFR-2-IN-39 inhibits the proliferation of EA.hy926, one of HUVECs, in a concentration-dependent manner, with an IC₅₀ of 38.65 µM.

PROTAC VEGFR-2 degrader-1 is a VEGFR-2-targeting PROTAC with >1 μM IC₅₀ against VEGFR-2, >100 μM IC₅₀ against endothelial cell proliferation, and no significant cytotoxicity against embryonic kidney cells. PROTAC VEGFR-2 degrader-1 can be used for the research of cancer.

VEGFR2 AUTOTAC-1 is a VEGFR2 AUTOTAC degrader. VEGFR2 AUTOTAC-1 recruits p62, activates the autophagy-lysosome pathway through the p62-LC3 axis cascade, forms a ternary complex with VEGFR2 and p62, and drives UPS-independent post-translational degradation of VEGFR2. VEGFR2 AUTOTAC-1 induces G1 phase arrest and endogenous apoptosis in cells via the mitochondrial and caspase apoptotic pathways, thereby inhibiting cancer cell proliferation, migration and malignant phenotypes; meanwhile, it inhibits endothelial cell tube formation, migration and endothelial-mesenchymal transition by regulating E-cadherin and MMP2. VEGFR2 AUTOTAC-1 is applicable to research related to triple-negative breast cancer.(Pink: VEGFR2 target protein ligand (HY-187558); Blue: E3 ligase ligand (HY-W014292); Black: Linker)

PROTAC VEGFR-2 degrader-2 is a VEGFR-2 (KDR) PROTAC degrader with weak inhibitory activity against VEGFR-2 (IC₅₀ > 1 μM). It is applicable to the research of cancer-related pathological angiogenesis.