MRT-2359 is a highly selective, orally bioavailable GSPT1 MGD designed through our QuEENTM platform Has optimal degradation kinetics to achieve preferential activity in MYC-driven cancer …

[2- (2,6-dioxopiperidin-3-yl)-3-oxo-1H-isoindol-5-yl]methyl N- [2-fluoro-5- (trifluoromethoxy)phenyl]carbamate | C22H17F4N3O6 | CID 164584214 - structure, chemical …

MRT-2359 is a GSPT1 MGD, which exploits this vulnerability by disrupting protein translation output and reducing MYC-oncogenic signaling leading to preferential anti-tumor activity in …

Preferential Activity of MRT-2359 in MYC-driven NSCLC Lines MRT-2359 induces GSPT1 degradation in all cell models, but shows preferential antiproliferative activity in high N-MYC …

MRT-2359 是一种有效、具有口服活性和选择性的 GSPT1 降解剂 (IC50: >30 nM 且 <300 nM)，能特异地诱导依赖于蛋白质翻译的细胞凋亡 (apoptosis)。 MRT-2359 在多种癌症细胞系中表现 …

2023年4月4日 · MRT-2359 was rationally designed using our QuEEN TM discovery engine and optimized to achieve a profound and preferential antiproliferative activity in MYC-driven cell …

Comment: MRT-2359 is a GSPT1 (a.k.a. eRF3a)-targeting molecular glue degrader. It uses a cereblon (CRBN) binding moiety to induce degradation of the translation termination factor …

MRT-2359's chemical structure was disclosed during the 'First Disclosures of New Drug Candidates' session at the April 2023 (Orlando) meeting of the AACR. An image of the ligand's …

2024年1月9日 · MRT-2359 is an orally active and potent degrader of GSPT1 with anti-tumor activity. MRT-2359 also inhibits the growth of resistant non-small cell lung cancer (NSCLC) …

MRT-2359是具有抗肿瘤活性的GSPT1的口服活性和强效降解剂。 MRT-2359还抑制耐药非小细胞肺癌 (NSCLC)和小细胞肺癌 (SCLC)细胞的生长。 MRT-2359在MYC驱动的细胞系中表现出优 …