Briciclib

• CAT Number: I005206
• CAS Number: 865783-99-9
• Molecular Formula: C19H23O10PS
• Molecular Weight: 474.42
• Purity: ≥95%
• Target: Cyclin D1
• Solubility: DMSO: ≥ 31 mg/mL
• Storage: Store at -20°C

Briciclib is a small molecule that suppresses cyclin D1 accumulation in cancer cells.Target: Cyclin D1in vitro: Briciclib inhibits the proliferation of MCL (JEKO-1 and MINO), breast (MCF7 and MDA-MB-231), gastric (AGS), and esophageal (OE19, OE33, and FLO-1) cancer cell lines at nanomolar concentrations (GI50 = 9.8 – 12.2 nM). [1] Cyclin D1 is a protein required for normal progression through the cell cycle and is overexpressed in many tumors. Cyclin D1 expression is regulated through a process termed cap-dependent translation, which requires the function of eukaryotic initiation factor 4E (eIF4E) protein. In vitro evidence indicates that briciclib binds to eIF4E, blocking cap-dependent translation of cyclin D1 and other cancer proteins (c-MYC, VEGF), leading to tumor cell death. Briciclib is potent and shown to be active in nonclinical tumor models when combined with several chemotherapeutics.

Reference

[1]. Neel Jasani, et al. Abstract 1649: Potent anticancer activity of an orally bioavailable small molecule, ON 013100, and its water soluble derivative, briciclib, a clinical-stage eIF4E-targeted agent. Cancer Res August 1, 201575; 1649