SBP-7455

• CAT Number: I036065
• CAS Number: 1884222-74-5
• Molecular Formula: C16H17F3N4O2
• Molecular Weight: 354.33
• Purity: 98%
• Solubility: Soluble in DMSO
• Storage: -20°C
• IUPAC Name: N4-cyclopropyl-N2-(3,4-dimethoxyphenyl)-5-(trifluoromethyl)pyrimidine-2,4-diamine
• InChI: InChI=1S/C16H17F3N4O2/c1-24-12-6-5-10(7-13(12)25-2)22-15-20-8-11(16(17,18)19)14(23-15)21-9-3-4-9/h5-9H,3-4H2,1-2H3,(H2,20,21,22,23)
• InChIKey: BQROJYIEHOOQBY-UHFFFAOYSA-N
• SMILES: COC1=C(OC)C=CC(NC2=NC(NC3CC3)=C(C(F)(F)F)C=N2)=C1

SBP-7455（Cat No.:I036065） is a dual inhibitor of ULK1 and ULK2 (ULK1/2), exhibiting enhanced binding affinity compared to SBI-0206965. It effectively inhibits the enzymatic activity of ULK1/2 both in vitro and in cells. SBP-7455 demonstrates potent reduction of viability in triple-negative breast cancer (TNBC) cells and displays oral bioavailability in mice. Moreover, it effectively suppresses starvation-induced autophagic flux in TNBC cells. These findings suggest that SBP-7455 holds potential as a therapeutic agent for TNBC by targeting the ULK1/2 pathway and regulating autophagy.

Reference

1: Ren H, Bakas NA, Vamos M, Chaikuad A, Limpert AS, Wimer CD, Brun SN, Lambert LJ, Tautz L, Celeridad M, Sheffler DJ, Knapp S, Shaw RJ, Cosford NDP. Design, Synthesis, and Characterization of an Orally Active Dual-Specific ULK1/2 Autophagy Inhibitor that Synergizes with the PARP Inhibitor Olaparib for the Treatment of Triple-Negative Breast Cancer. J Med Chem. 2020 Nov 17. doi: 10.1021/acs.jmedchem.0c00873. Epub ahead of print. PMID: 33200929.