SBP-7455 是一种有效的、高亲和力和口服活性的双重 ULK1/ULK2 自噬抑制剂，在 ADP-Glo 试验中 IC50 分别为 13 nM 和 476 nM。 SBP-7455 有效抑制 ULK1/2 酶活性，可用于三阴性乳腺癌 (TNBC) 研究。
货号:ajcx24460
CAS:1884222-74-5
分子式:C16H17F3N4O2
分子量：354.3
溶解度:DMF: 30 mg/ml,DMSO: 30 mg/ml,DMSO:PBS (pH 7.2) (1:4): 0.20 mg/ml,Ethanol: 1 mg/ml
纯度：98%
存储：Store at -20°C
库存：现货

Background:

SBP-7455 is a dual inhibitor of unc-51-like autophagy activating kinase 1 (ULK1) and ULK2 (IC₅₀s = 13 and 476 nM, respectively, for the recombinant human enzymes in cell-free assays).¹It inhibits increases in autophagic flux and induces apoptosis in serum-deprived MDA-MB-468 breast cancer cells when used at a concentration of 10 µM. SBP-7455 (0.19 µM), alone or in combination with olaparib , reduces the viability of MDA-MB-468 cells.

1.Ren, H., Bakas, N.A., Vamos, M., et al.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 cancerJ. Med. Chem.63(23)14609-14625(2020)