PROTAC PD-1/PD-L1 degrader-1，基于 Cereblon E3配体的 PD-1/PD-L1 PROTAC，抑制 PD-1/PD-L1 相互作用，IC50 为 39.2 nM。PROTAC PD-1/PD-L1 degrader-1 可显着恢复在 Hep3B/OS-8/hPD-L1 和 CD3 T 细胞共培养模型中抑制的免疫力。PROTAC PD-1/PD-L1 degrader-1 以溶酶体依赖性方式适度降低 PD-L1 的蛋白质水平。
货号:ajcx35876
CAS:2447066-37-5
分子式:C59H58ClN7O11
分子量：1076.59
溶解度:DMSO : 210 mg/mL (195.06 mM; Need ultrasonic)
纯度：98%
存储：Store at -20°C
库存：现货

Background:

PROTAC PD-1/PD-L1 degrader-1, a PD-1/PD-L1 PROTAC based on Cereblon E3 ligand, inhibits PD-1/PD-L1 interaction with an IC50 of 39.2 nM. PROTAC PD-1/PD-L1 degrader-1 significantly restores the immunity repressed in a co-culture model of Hep3B/OS-8/hPD-L1 and CD3 T cells. PROTAC PD-1/PD-L1 degrader-1 moderately reduces the protein levels of PD-L1 in a lysosome-dependent manner[1].

PROTAC PD-1/PD-L1 degrader-1 (compound p22) reduces cell surface PD-L1 expression for more than 14%[1].PROTAC PD-1/PD-L1 degrader-1 (1-10 μM; 24 hours) reduces PD-L1 expression in a dose-dependent manner by 21% and 35% at 1 μM and 10 μM, respectively[1].

[1]. Cheng B, Ren Y, Cao H, Chen J. Discovery of novel resorcinol diphenyl ether-based PROTAC-like molecules as dual inhibitors and degraders of PD-L1. Eur J Med Chem. 2020;199:112377.