Product Description: XYD049 (compound 7d) is a CRBN-type molecular glue targeting GSPT1 (DC50=19 nM), which can be used for the research of MYC-driven castration-resistant prostate cancer (CRPC). XYD049 can effectively inhibit the growth of 22Rv1 cells (IC50=7 nM) and has in vivo antitumor efficacy. XYD049 downregulates the CRPC-related oncogenes in 22Rv1 cells, including AR, AR-v7, PSA, and c-Myc. XYD049 is composed of a molecular glue linker (black part) NH2-C5-NH-Boc (HY-W004710), a CRBN-type E3 ligase ligand (blue part) Thalidomide 4-fluoride (HY-41547), and a target protein ligand (red part) GSPT1 ligand-1 (HY-170821), in which the E3 ligase ligand + liner form a conjugate E3 Ligase Ligand-linker Conjugate 158 (HY-170822)[1].
Applications: Cancer-programmed cell death
Formula: C35H35BrN6O10S
References: [1]Shen H, et al. Discovery of a Potent and Selective GSPT1 Molecular Glue Degrader for the Treatment of Castration-Resistant Prostate Cancer. J Med Chem. 2025 Jan 23;68(2):1553-1571.
CAS Number: 3006788-11-7
Molecular Weight: 811.66
Research Area: cancer
Target: Molecular Glues
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