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- PROTAC PD-1/PD-L1 degrader-1
PROTAC PD-1/PD-L1 degrader-1
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。
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包装价格促销价数量
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5mg￥9500.007600.00- +
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10mg￥14962.0011970.00- +
- 货号: ajcx35876
- CAS: 2447066-37-5
- 别名:
- 分子式: C59H58ClN7O11
- 分子量: 1076.59
- 纯度: ＞98%
- 溶解度: DMSO : 210 mg/mL (195.06 mM; Need ultrasonic)
- 储存: Store at -20°C, sealed storage, away from moisture and light
- 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.
