INCB086550

• CAT Number: I044532
• CAS Number: 2230911-59-6
• Molecular Formula: C41H39N7O4
• Molecular Weight: 693.79
• Purity: ≥95%
• Synonyms: (3R)-1-[[7-cyano-2-[3-[3-[[3-[[(3R)-3-hydroxypyrrolidin-1-yl]methyl]-1,7-naphthyridin-8-yl]amino]-2-methylphenyl]-2-methylphenyl]-1,3-benzoxazol-5-yl]methyl]pyrrolidine-3-carboxylic acid
• InChI: InChI=1S/C41H39N7O4/c1-24-32(5-3-7-34(24)40-46-36-17-26(15-30(18-42)38(36)52-40)20-47-13-10-29(22-47)41(50)51)33-6-4-8-35(25(33)2)45-39-37-28(9-12-43-39)16-27(19-44-37)21-48-14-11-31(49)23-48/h3-9,12,15-17,19,29,31,49H,10-11,13-14,20-23H2,1-2H3,(H,43,45)(H,50,51)/t29-,31-/m1/s1
• InChIKey: QARLNMDDSQMINK-BVRKHOPBSA-N
• SMILES: CC1=C(C=CC=C1C2=NC3=CC(=CC(=C3O2)C#N)CN4CCC(C4)C(=O)O)C5=C(C(=CC=C5)NC6=NC=CC7=CC(=CN=C76)CN8CCC(C8)O)C

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[1].
INCB086550 (0.1-10000 nM, 20 h) has no overt toxicity to pleural effusion fluids cells[1].
INCB086550 (1 µmol/L, 24 h) induces the dimerization of cell-surface PD-L1 and resulting in internalization[1].
INCB086550 (15, 200 mg/kg for Oral gavage, once or twice) inhibits greater than 90% of unoccupied cell surface PD-L1 in MDA-MB-231 mice model[1].
INCB086550 (2, 20, or 200 mg/kg for Oral gavage, b.i.d) inhibits tumor growth in MC38 huPD-L1 mice model[1].

Reference

[1]. WU LIANGXING, et al. BENZOOXAZOLE DERIVATIVES AS IMMUNOMODULATORS. WO2018119266A1.

[2]. Koblish HK, et al. Characterization of INCB086550: A Potent and Novel Small-Molecule PD-L1 Inhibitor. Cancer Discov. 2022 Jun 2;12(6):1482-1499.
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