INCB086550 | PD-1/PD-L1 inhibitor | Probechem Biochemicals

Chemical Structure : INCB086550

CAS No.: 2230911-59-6

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INCB086550 (INCB86550, INCB 086550)

货号: PC-72848Not For Human Use, Lab Use Only.

INCB086550 (INCB 086550) is a potent, selective small-molecule inhibitor of PD-L1, inhibits PD-L1/PD-1 interaction with IC50 of 3.1, 4.9 and 1.9 nM for human, cynomolgus and rat PD-L1 in HTRF-based assays.

规格	价格	库存
5 mg	￥2480	In stock
10 mg	￥3980	In stock
25 mg	￥5880	In stock
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100 mg		Get quote

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生物&药学活性

INCB086550 (INCB 86550) is a potent, selective small-molecule inhibitor of PD-L1, inhibits PD-L1/PD-1 interaction with IC50 of 3.1, 4.9 and 1.9 nM for human, cynomolgus and rat PD-L1 in HTRF-based assays.
INCB086550 inhibited binding of phycoerythrin (PE)-labeled PD-1 (PD-1/PE) to cell surface PD-L1 with IC50 of 13 nM.
INCB086550 blocked binding of the clinical anti–PD-L1 monoclonal antibodies (mAbs), atezolizumab and durvalumab, to PD-L1, potently and selectively binds to PD-L1 at a site that overlaps with the clinical anti-PD-L1 mAbs.
INCB086550 binds to PD-L1 and interrupts its interaction with PD-1 and also induces PD-L1 dimerization and internalization.
INCB086550 effectively restored NFAT pathway activation and abolished SHP recruitment to PD-1, thereby demonstrating functional 346 inhibition of the PD-L1/PD-1 signaling pathway.
INCB086550 dose-dependently reduced unoccupied cell surface PD-L1 on the tumor cell surface in vivo, effectively inhibited tumor growth as a single agent in multiple humanized tumor models and was well tolerated.
INCB086550 reduced tumor growth in CD34+ humanized mice and induced T-cell activation gene signatures, consistent with PD-L1/PD-1 pathway blockade in vivo.
Oral administration of INCB086550 provides dose-related pharmacodynamic immune activation similar to that reported for PD-L1 or PD-1 therapeutic antibodies.

物理化学性质&存储条件

分子量	693.808
分子式	C41H39N7O4
外观性状	Solid
CAS No.
储存条件	固体粉末 -20°C 12 个月; 4°C 6 个月	配置液 -80°C 6 个月; -20°C 6 个月
Shipping
Solubility	10 mM in DMSO
Chemical Name/SMILES	(S)-1-((7-cyano-2-(3'-((3-(((S)-3-hydroxypyrrolidin-1-yl)methyl)-1,7-naphthyridin-8-yl)amino)-2,2'-dimethyl-[1,1'-biphenyl]-3-yl)benzo[d]oxazol-5-yl)methyl)pyrrolidine-3-carboxylic acid

参考文献

1. Holly K Koblish, et al. Cancer Discov. 2022 Mar 7;candisc.1156.2021.

INCB086550 (INCB86550, INCB 086550)

生物&药学活性

物理化学性质&存储条件

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INCB086550 (INCB86550, INCB 086550)

生物&药学活性

物理化学性质&存储条件

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