gefitinib based protac 3

Gefitinib-based PROTAC 3 通过 linker 将 EGFR 结合元件与 von Hippel-Lindau 配体结合，在 HCC827（外显子 19 del）和 H3255（L858R 突变）细胞中诱导 EGFR 降解，DC50 分别为 11.7 和 22.3 nM。

PROTACFLT-3degrader 4 是一种口服活性强的 CRBN 基于的 FLT3-PROTAC 降解剂，能够通过泛素-蛋白酶体系统有效降解 FLT3-ITD。此化合物对 FLT3-ITD 突变的急性髓性白血病 (AML) 细胞展现出高度选择性。

PROTACBcl-xL degrader-3 是一种有效的 PROTACBcl-xL 降解剂。

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

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].

PROTACEGFRdegrader 3 是一种有效的 PROTACEGFR 降解剂。PROTACEGFRdegrader 3 对 H1975 和 HCC827 细胞具有优异的细胞活性和高选择性。PROTACEGFRdegrader 3 表明溶酶体参与了 EGFR 突变体的降解过程。

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

PROTAC BET Degrader-3 is a potent degrader of BET proteins based on the PROTAC (PROteolysis TArgeting Chimera) technology.

PROTACSOS1 degrader-3 是一种有效的 PROTACSOS1降解剂。PROTACSOS1 degrader-3 通过泛素-蛋白酶体系统有效靶向 SOS1 进行降解。

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

PROTACIRAK4 ligand-3 为 PROTACIRAK4 degrader-7 配体，适用于癌症研究领域。

PROTACBRD9 Degrader-3为BRD9靶向的双功能降解剂，用于癌症研究。

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

PROTACSMARCA2 degrader-3(Compound 153)作为SWI SNF ATPase亚基SMARCA2的PROTAC降解剂，展现出抗癌活性。

PROTACα-synuclein degrader 3 (compound 5) 为高效的选择性 PROTACα-synuclein 降解剂，适用于帕金森病研究。

PROTACBTK Degrader-3为BTKPROTAC降解剂，具有效力，其在Mino细胞中BTK降解的DC50值为10.9 nM。该降解剂具有应用于研究B细胞恶性肿瘤潜力，包括慢性淋巴细胞恶性肿瘤。