PD-L1-IN-1 是一种有效的 PD-L1 抑制剂，IC50 为 115 nM。PD-L1-IN-1与PD-L1蛋白强结合，并在表达 PD-L1 的癌细胞（PC9 和 HCC827 细胞）和外周血单核细胞的共同培养中激发 PD-L1 蛋白，增强后者的抗肿瘤免疫活性。PD-L1-IN-1 显著增加了干扰素 γ 的释放和癌细胞的凋亡诱导，对健康细胞的细胞毒性较低。
货号:ajcx36744
CAS:N/A
分子式:C21H23N5O2
分子量：377.44
溶解度:DMSO : 125 mg/mL (331.18 mM; ultrasonic and warming and heat to 60°C)
纯度：98%
存储：Store at -20°C
库存：现货

Background:

PD-L1-IN-1 is a potent PD-L1 inhibitor with an IC50 of 115 nM. PD-L1-IN-1 strongly binds with the PD-L1 protein and challenged it in a co-culture of PD-L1 expressing cancer cells (PC9 and HCC827 cells) and peripheral blood mononuclear cells enhanced antitumor immune activity of the latter. PD-L1-IN-1 significantly increased interferon γ release and apoptotic induction of cancer cells, with low cytotoxicity in healthy cells[1].

[1]. Russomanno P, et al. Interfering with the Tumor-Immune Interface: Making Way for Triazine-Based Small Molecules as Novel PD-L1 Inhibitors. J Med Chem. 2021;64(21):16020-16045.