MRT-2359

Overview

MRT-2359 is an orally active and selective GSPT1 molecular glue degrader, with a DC 50 of 5 nM. MRT-2359 induces CRBN /GSPT1 ternary complex formation to drive CRBN- and degron-dependent proteasomal GSPT1 degradation, with selectivity for wild-type GSPT1 over the GSPT1 G575N mutant. MRT-2359 disrupts protein translation, induces ribosome stalling, downregulates MYC family proteins and their transcriptional output, reduces proliferation, and induces apoptosis in cancer cells. MRT-2359 can be used for the research of non-small cell lung cancer (NSCLC), small cell lung cancer (SCLC), neuroendocrine lung cancer , high grade neuroendocrine cancers, diffuse large B-cell lymphoma, prostate cancer , and MYC -driven solid tumors.

Application

Products | Products > Disease Areas > Urogenital Disease | Products > Disease Areas > Digestive System Disease | Products > Disease Areas > Lung Cancer | Products > Disease Areas > Respiratory Cancer | Products > Disease Areas > Leukemia/Lymphoma/Myeloma | Products > Disease Areas > Prostate Cancer | Products > Disease Areas > Urogenital Cancer | Products > Disease Areas > Blood Disease | Products > Disease Areas > Digestive System Inflammation | Products > Disease Areas > Small Cell Lung Cancer | Products > Disease Areas > Non-Small Cell Lung Cancer | Products > Disease Areas > Diffuse Large B-cell Lymphoma | Products > Disease Areas > Cancer | Products > Disease Areas > Blood or Cardio-cerebrovascular Disease | Products > Disease Areas > Inflammation or Immune System Disease | Products > Disease Areas > Respiratory Disease | Products > Signaling Pathways > PROTAC | Products > Signaling Pathways > Apoptosis | Products > Research Areas > Inflammation/Immunology | Products > Research Areas > Cancer | Products > Research Areas > Cancer > Cancer Targeted Therapy | Products > Research Areas > Cancer > Cancer Drug Resistance | Products > Research Areas > Cancer > Cancer Metabolism and Metastasis | Products > Signaling Pathways > Molecular Glues | Products > Signaling Pathways > Apoptosis

Product Information

• Catalog No.: HY-153356
• CAS No.: 2803881-11-8
• Molecular Formula: C22H17F4N3O6
• Molecular Weight: 495.38
• Purity: 99.91%
• Storage: Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 6 months , -20°C, 1 month
• Solubility: 2.5 mg/mL (5.05 mM); Suspended solution; Need ultrasonic
• Availability: In-stock

Source

Original product source