Formulation: A solid
Formal Name: (3R)-1-[[7-cyano-2-[3′-[[3-[[(3R)-3-hydroxy-1-pyrrolidinyl]methyl]-1,7-naphthyridin-8-yl]amino]-2,2′-dimethyl[1,1′-biphenyl]-3-yl]-5-benzoxazolyl]methyl]-3-pyrrolidinecarboxylic acid
Purity: ≥98%
Formula Markup: C41H39N7O4
Formula Weight: 693,8
Shelf life (days): 1460
CAS Number: 2230911-59-6
Notes: INCB 086550 is an inhibitor of the protein-protein interaction between programmed cell death 1 (PD-1) and its ligand PD-L1.{65881} It inhibits PD-1 binding to PD-L1 in CHO cells expressing human PD-L1 (EC50 = 13.2 nM). INCB 086550 (1 µM) induces dimerization and internalization of PD-L1 in CHO cells expressing human PD-L1. It decreases the levels of unoccupied cell-surface PD-L1 in mouse MBT-2 bladder cancer cells expressing human PD-L1 at low, medium, or high levels (EC50s = 3.7, 0.4, and 0.1 nM, respectively). It prevents PD-1-induced recruitment of Src homology region 2 domain-containing phosphatase (SHP) in a reporter assay using Jurkat T cells co-cultured with U2OS cells expressing human PD-L1 (IC50 = 6.3 nM) and induces activation of nuclear factor of activated T cells (NFAT) in a reporter assay using Jurkat T cells co-cultured with CHO-K1 cells (IC50 = 21.4 nM). In vivo, INCB 086550 (20 or 200 mg/kg per day) reduces tumor volume and intratumoral cell-surface levels of PD-L1, as well as increases CD8+ T cell tumor infiltration, in an MC-38 murine allograft model of colon carcinoma overexpressing human PD-L1 (MC-38-hPD-L1).
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