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。
| Cas No. | 1884222-74-5 |
| Canonical SMILES | FC(F)(C1=CN=C(NC2=CC=C(C(OC)=C2)OC)N=C1NC3CC3)F |
| 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 |
| 储存条件 | -20°C |
| General tips | For obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while. |
| Shipping Condition | Evaluation sample solution : ship with blue ice
All other available size: ship with RT , or blue ice upon request |
| 产品描述 | 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) |
