gefitinibbased protac 3

PROTAC Bcl-xL degrader-3 is a potent ROTAC Bcl-xL degrader.

PROTAC EGFR Degrader 3, a highly potent molecule, exhibits remarkable cellular activity against H1975 and HCC827 cells, maintaining high selectivity. It additionally reveals the lysosome's crucial role in the degradation mechanism of mutant EGFR [1].

PROTAC FLT-3 degrader 1 is a PROTAC FLT-3 degrader of internal tandem duplication (ITD)(IC50 0.6 nM),with anti-proliferative activity.

PROTAC IRAK4 Ligand-3 serves as a ligand for PROTAC IRAK4 Degrader-7 and is utilized in cancer research [1].

PROTAC BRD9 Degrader-3 is a bifunctional degrader targeting BRD9, utilized in cancer research.

PROTAC BTK Degrader-3 is a potent degrader of Bruton's tyrosine kinase (BTK), exhibiting a DC50 (median degradation concentration) of 10.9 nM in Mino cells. This compound shows promise for research into B-cell malignancies, such as chronic lymphoid malignancies [1].

Gefitinib-based PROTAC 3, conjugating an EGFR binding element to a VHL ligand via a linker, induces EGFR degradation with DC50s of 11.7 nM and 22.3 nM in HCC827(exon 19 del) and H3255 (L858R mutantion) cells, respectively[1].

PROTAC MDM2 Degrader-3 is a compound that leverages PROTAC technology to degrade MDM2. It consists of a highly effective MDM2 inhibitor, a linker, and the MDM2 ligand for E3 ubiquitin ligase[1].

PROTAC ER Degrader-3, an intermediate for the synthesis of PAC, specifically compound LP2. PAC serves as the linker for ADCs and PROTACs that are conjugated to an antibody. Notably, when PAC is conjugated to an antibody, it exhibits enhanced degradation of estrogen receptor-alpha (ERα) compared to PROTAC alone [1].

PROTAC BRD4 Degrader-3 is an efficacious degrader of PROTAC BRD4.

PROTAC BET Degrader-3 is a potent degrader OF BET based on PROTAC.

PROTAC SOS1 Degrader-3 is a potent agent specifically designed to target and degrade SOS1 via the ubiquitin-proteasome system [1].

PROTAC IRAK4 degrader-3 is a PROTAC-induced IRAK4 degrader based on von Hippel-Lindau.

PROTAC FKBP Degrader-3 is a PROTAC that comprises a FKBP ligand binding group, a linker and an VHL binding group. PROTAC FKBP Degrader-3 is a potent FKBP degrader[1].

PROTAC ERRα Degrader-3 is a highly effective and selective von Hippel-Lindau-based ligand that efficiently degrades the ERRα protein. At a concentration of 30 nM, this compound exhibits a remarkable degradation capability, reducing the ERRα protein levels by >80%. Importantly, PROTAC ERRα Degrader-3 shows no activity against the ERRβ and ERRγ proteins.

PROTAC CRABP-II Degrader-3 is a potent degrader of cellular retinoic acid binding protein (CRABP-II) based on cIAp1.

PROTAC α-synuclein degrader 3 (compound 5) serves as a potent and selective agent for degrading α-synuclein and is utilized in Parkinson's disease research [1].