TABLE 1

Inhibitory activity of INCB040093 against human primary immune cell

Primary CellStimulantResponseIC50 (nM)a
B (CD21+; canine)Anti-dog IgMProliferation2.1 ± 0.01
B (CD19+; human)Anti-human IgMProliferation2.4 ± 0.5
B (CD19+; human)LPSProliferation0.9 ± 0.3
B (CD19+; human)IL-4Proliferation3.8 ± 2.1
B (CD19+; human)IL-6Proliferation1.7 ± 0.3
B (CD19+; human)BAFFProliferation1.2 ± 0.8
B (CD19+; human)Anti-CD40Proliferation3.2 ± 1.0
B (CD19+; human)CD40 ligandProliferation2.8 ± 1.8
BasophilbAnti-Fcε receptorCD63 expression35 ± 15
T (CD4+CD45RA+, human)Th17 cocktailcTh17 differentiation3.9 ± 3
T (total T cellsd, human)Anti-CD3Proliferation2133 ± 1122
T (total T cellsd, human)Anti-CD28Proliferation130 ± 31
T (total T cellsd, human)Anti-CD28 and anti-CD3Proliferation1753 ± 632
T (CD3+, human)IL-2Proliferation3107 ± 1371
NK (CD56+, human)IL-2Proliferation708 ± 50
Neutrophil (human)fMLPElastase exocytosis1566 ± 545
PBMC (human)LPSTNF-α production2704 (n = 1)
Monocytes (human)CCL2Chemotaxis>10,000
  • a The data represent IC50 ± S.D.

  • b The assay was done in the presence of human whole blood.

  • c IL-1β, IL-6, IL-23, transforming growth factor-β, anti–interferon-β, and anti–IL-4 antibodies.

  • d PBMC elutriation fraction 2000.