DAS-5-oCRBN

Overview

DAS-5-oCRBN is a PROTAC molecule with both c‑Src kinase inhibitory activity and target protein degradation activity, with an EC 50 of 45 nM for c‑Src binding. DAS-5-oCRBN binds non-covalently to Cereblon and mediates target protein degradation via the ubiquitin-proteasome pathway. DAS-5-oCRBN can catalytically deplete intracellular c‑Src protein, while blocking both the kinase catalytic function of c‑Src and the non-catalytic protein interactions mediated by its SH2 and SH3 domains. DAS-5-oCRBN inhibits tumor cell proliferation and exerts significant anti-proliferative effects on both c‑Src kinase activity-dependent MDA-MB-231 cells and c‑Src protein level-dependent CAL51 cells. DAS-5-oCRBN can be used in cancer-related research such as studies on triple-negative breast cancer and chronic myeloid leukemia. (Pink: c-Src ligand ( HY-107447 ); Blue: Cereblon ligand ( HY-148834 ); Black: linker).

Application

Products | Products > Disease Areas > Blood Disease | Products > Disease Areas > Triple-Negative Breast Cancer | Products > Disease Areas > Cancer | Products > Disease Areas > Blood or Cardio-cerebrovascular Disease | Products > Disease Areas > Breast Cancer | Products > Disease Areas > Leukemia/Lymphoma/Myeloma | Products > Signaling Pathways > PROTAC | Products > Signaling Pathways > Protein Tyrosine Kinase/RTK | Products > Research Areas > Cancer | Products > Research Areas > Cancer > Cancer Targeted Therapy | Products > Research Areas > Cancer > Cancer Immunotherapy | Products > Signaling Pathways > PROTACs | Products > Signaling Pathways > Src

Product Information

• Catalog No.: HY-163144
• CAS No.: 3044084-97-8
• Molecular Formula: C39H40ClN11O6S
• Molecular Weight: 826.32
• Purity: 99.21%
• 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 (3.03 mM); Clear solution
• Availability: In-stock

Source

Original product source