产品
编 号：F741442
分子式：C41H39N7O4
分子量：693.79
分子式：C41H39N7O4
分子量：693.79
产品类型
规格
价格
是否有货
1mg
询价
询价
5mg
询价
询价
10mg
询价
询价
25mg
询价
询价
结构图
CAS No: 2230911-59-6
产品详情
生物活性：
INCB086550 is a potent, oral, small-molecule PD-L1 inhibitor with IC50s value of 3.1, 4.9 and 1.9 nM for human, cynomolgus, and rat, respectively. INCB086550 promotes the dimerization of cell-surface PD-L1 and induces PD-L1 entry into Golgi vesicles then traffick to the nucleus. INCB086550 can be used for multiple cancers research.
体内研究：
INCB086550 (15, 200 mg/kg，口服给药，一次或两次) 抑制MDA-MB-231小鼠模型中 90% 以上未被占用的细胞表面 PD-L1。INCB086550 (2, 20, or 200 mg/kg，口服给药，每天两次) 抑制 MC38 huPD-L1 小鼠模型的肿瘤生长。Animal Model:mice bearing MDA-MB-231 xenografts
Dosage:15, 200 mg/kg
Administration:Oral gavage (p.o.)
Result:Reduced unoccupied cell-surface PD-L1 on MDA-MB-231 tumors at 24 hours.
Animal Model:C57BL/6 and NSG mice bearing established MC38-huPD-L1 tumors
Dosage:2, 20, or 200 mg/kg
Administration:Oral gavage (p.o.)
Result:Induced a dose-dependent decrease of PD-L1 available to bind to PD-1 using antibody clone MIH1.Reduced occupied cell-surface PD-L1 > 90% at the 200 mg/kg dose.
体外研究：
INCB086550 (0.1-10000 nM, 20小时) 对胸腔积液细胞无明显毒性。NCB086550 (1 μmol/L, 24小时) 诱导细胞表面PD-L1的二聚化并导致内化。
INCB086550 is a potent, oral, small-molecule PD-L1 inhibitor with IC50s value of 3.1, 4.9 and 1.9 nM for human, cynomolgus, and rat, respectively. INCB086550 promotes the dimerization of cell-surface PD-L1 and induces PD-L1 entry into Golgi vesicles then traffick to the nucleus. INCB086550 can be used for multiple cancers research.
体内研究：
INCB086550 (15, 200 mg/kg，口服给药，一次或两次) 抑制MDA-MB-231小鼠模型中 90% 以上未被占用的细胞表面 PD-L1。INCB086550 (2, 20, or 200 mg/kg，口服给药，每天两次) 抑制 MC38 huPD-L1 小鼠模型的肿瘤生长。Animal Model:mice bearing MDA-MB-231 xenografts
Dosage:15, 200 mg/kg
Administration:Oral gavage (p.o.)
Result:Reduced unoccupied cell-surface PD-L1 on MDA-MB-231 tumors at 24 hours.
Animal Model:C57BL/6 and NSG mice bearing established MC38-huPD-L1 tumors
Dosage:2, 20, or 200 mg/kg
Administration:Oral gavage (p.o.)
Result:Induced a dose-dependent decrease of PD-L1 available to bind to PD-1 using antibody clone MIH1.Reduced occupied cell-surface PD-L1 > 90% at the 200 mg/kg dose.
体外研究：
INCB086550 (0.1-10000 nM, 20小时) 对胸腔积液细胞无明显毒性。NCB086550 (1 μmol/L, 24小时) 诱导细胞表面PD-L1的二聚化并导致内化。
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