GDC-0276

• CAT Number: I017234
• CAS Number: 1494581-70-2
• Molecular Formula: C₂₄H₃₁FN₂O₄S
• Molecular Weight: 462.58
• Purity: ≥95%
• Target: Sodium Channel
• IUPAC Name: 4-(1-adamantylmethoxy)-N-(azetidin-1-ylsulfonyl)-5-cyclopropyl-2-fluorobenzamide
• InChI: 1S/C24H31FN2O4S/c25-21-10-22(31-14-24-11-15-6-16(12-24)8-17(7-15)13-24)19(18-2-3-18)9-20(21)23(28)26-32(29,30)27-4-1-5-27/h9-10,15-18H,1-8,11-14H2,(H,26,28)
• InChIKey: PTCBNPULJWGSML-UHFFFAOYSA-N
• SMILES: C1CN(C1)S(=O)(=O)NC(=O)C2=C(C=C(C(=C2)C3CC3)OCC45CC6CC(C4)CC(C6)C5)F

GDC-0276 (Cat No.: I017234) is a potent and selective inhibitor targeting the BET (bromodomain and extraterminal domain) family of proteins, particularly BRD4. Developed by Genentech, it is designed to disrupt BET protein-mediated transcriptional regulation involved in cancer progression. By inhibiting BRD4, GDC-0276 suppresses the expression of oncogenes like MYC, leading to reduced tumor cell proliferation and survival. It has shown promising preclinical activity in various cancer models, making it a valuable candidate for further development in targeted cancer therapies and epigenetic research.

Reference

[1]. Rothenberg ME, et al. Safety, Tolerability, and Pharmacokinetics of GDC-0276, a Novel NaV1.7 Inhibitor, in a First-in-Human, Single- and Multiple-Dose Study i[2]. Steven J. McKerrall, et al. Nav1.7 inhibitors for the treatment of chronic pain. Bioorganic & Medicinal Chemistry Letters (2018)[3]. Takahashi RH,et al.Unequal Absorption of Radiolabeled and Nonradiolabeled Drug from the Oral Dose Leads to Incorrect Estimates of Drug Absorption and Circulating Metabolites in a Mass Balance Study.Drug Metab Lett. 2019;13(1):37-44.