INCB086550

本公司产品仅用于科研实验，不得用于人体或动物的临床与诊断

INCB086550 是一种强效的口服小分子 PD-L1 抑制剂，其对人、食蟹猴和大鼠的 PD-L1 IC50 值分别为 3.1, 4.9 和 1.9 nM。INCB086550 促进细胞表面 PD-L1 二聚化，并诱导 PD-L1 进入高尔基囊泡，随后转运到细胞核。INCB086550 可用于多种癌症疾病的研究。

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.

Cell Viability Assay Cell Line:Pleural effusion fluids cells Concentration:0.1-10000 nM Incubation Time:20 h Result:Had no overt toxicity to pleural effusion fluids cells. Immunofluorescence Cell Line:CHO PD-L1 cells Concentration:1 μmol/L Incubation Time:24 h Result:Decreased overall PD-L1 in CHO PD-L1 cells. Demonstrated rapid internalization of PD-L1 that appeared maximal about 4 hours.

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.

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Immunology/Inflammation

PD-1/PD-L1

PD-1/PD-L1

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2230911-59-6

693.79

C41H39N7O4

>98% (HPLC)

In Vitro:?H2O 中的溶解度 : 83.33 mg/mL (120.11 mM; 超声助溶 酸性条件溶解 (HCL 调节，pH≈3))

Cc1c(Nc2nccc3cc(CN4CC[C@@H](O)C4)cnc23)cccc1-c1cccc(-c2nc3cc(CN4CC[C@H](C4)C(O)=O)cc(C#N)c3o2)c1C

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(-20℃)

With Ice Pack

≥ 2 years