protac k-ras degrader-1

PROTAC K-Ras Degrader-1 是一种基于 Cereblon E3 配体的 PROTAC 降解剂，可降解 K-Ras。

K-Ras ligand-Linker Conjugate 1 is a chemical compound that includes a ligand for K-Ras and a PROTAC linker, facilitating the recruitment of E3 ligases VHL, CRBN, MDM2, and IAP. It can be utilized in the synthesis of PROTAC K-Ras Degrader-1, a highly effective K-Ras degrader that achieves ≥70% degradation efficacy in SW1573 cells[1].

K-Ras ligand-Linker Conjugate 2 is a chemical compound that includes a ligand for K-Ras and a PROTAC linker. This compound is capable of recruiting E3 ligases like VHL, CRBN, MDM2, and IAP. It is utilized in the synthesis of PROTAC K-Ras Degrader-1, which is a highly effective PROTAC K-Ras degrader with a degradation efficacy of ≥70% in SW1573 cells[1].

K-Ras ligand-Linker Conjugate 3 (Compound 001371) is a chemical compound that consists of a ligand for K-Ras recruiting moiety and a PROTAC linker, responsible for recruiting E3 ligases (e.g., VHL, CRBN, MDM2, and IAP). This compound is essential in the synthesis of PROTAC K-Ras Degrader-1, a potent PROTAC K-Ras degrader that demonstrates a degradation efficacy of ≥70% in SW1573 cells[1].

K-Ras ligand-Linker Conjugate 4 is a chemical compound that combines a ligand for K-Ras recruiting moiety with a PROTAC linker. This linker is responsible for recruiting E3 ligases such as VHL, CRBN, MDM2, and IAP. The compound has the potential to be used in the synthesis of PROTAC K-Ras Degrader-1, a powerful degrader of K-Ras that has been shown to exhibit a degradation efficacy of ≥70% in SW1573 cells[1].

K-Ras ligand-Linker Conjugate 5 is a chemical compound that combines a ligand for the K-Ras recruiting moiety with a PROTAC linker. This linker is responsible for recruiting E3 ligases such as VHL, CRBN, MDM2, and IAP. The K-Ras ligand-Linker Conjugate 5 plays a crucial role in the synthesis of PROTAC K-Ras Degrader-1, a highly potent K-Ras degrader. In SW1573 cells, this degrader exhibits an impressive degradation efficacy of ≥70% [1].

K-Ras ligand-Linker Conjugate 6 是一种结合 K-Ras 招募片段配体和PROTAC连接子的化合物,可募集 E3 连接酶,合成 PROTAC K-Ras Degrader-1.

THP-PEG4-Pyrrolidine(N-Boc)-CH2OH is a polyethylene glycol (PEG) based PROteolysis TArgeting Chimera (PROTAC) linker, employed for the synthesis of PROTAC K-Ras Degrader-1, as documented in reference [1].

THP-PEG4-Pyrrolidine(N-Me)-CH2OH, a PEG-based PROTAC linker, facilitates the synthesis of PROTAC K-Ras Degrader-1[1].

Tos-PEG4-THP is a polyethylene glycol (PEG) derivative utilized as a linker in the synthesis of PROTAC K-Ras Degrader-1, a potential therapeutic compound for targeted degradation of K-Ras protein [1].

PROTAC K-Ras Degrader-4是一种PROTAC分子，可以选择性降解致癌突变体K-Ras，在GP5d细胞系中有效降解KRASG12D，在SW620细胞中有效降解KRASG12V，DC50分别为1和13nM。PROTAC K-Ras Degrader-4同时抑制下游MAPK信号通路，这使其成为了了一种针对先前不可成药的Ras突变癌症的新研究策略。

K-Rasligand-Linker Conjugate 6 formate 包含靶标K-Ras配体 (K-Ras募集基序) 以及PROTAClinker，可招募E3连接酶 [如VHL, CRBN, MDM2和IAP等]。K-Rasligand-Linker Conjugate 6 适用于合成PROTACK-Ras Degrader-1，一种高效的PROTACK-Ras降解剂，在SW1573细胞中对K-Ras降解率达到或超过70%。

PROTAC KRAS G12C degrader-2（compound 432）是一种靶向调控 K-Ras 蛋白水解的双功能 PROTAC 分子，一端包含 cereblon/IAP 配体，另一端为 KRAS 结合基团，可选择性募集突变型 KRAS G12C 至泛素–蛋白酶体系统中进行降解，用于研究 KRAS 驱动型致瘤信号通路的机制。