Table 2.
In vitro characteristics of NTRC 3883-0 and epacadostat.
| Assay | NTRC 3883-0 | epacadostat |
|---|---|---|
| hIDO1 | 123 (116–130) (n = 85) | 27 (25–29) (n = 91) |
| hTDO | < 20% inhibition @ 31,600 (n = 82) | 54 (50–58) (n = 89) |
| HEK-hIDO1 | 119 (n = 2) | 7.9 (n = 2) |
| HEK-hTDO | < 20% inhibition @ 31,600 (n = 2) | 24,100 (n = 2) |
| A375 + IFNγ (hIDO1) | 182 (155–214) (n = 63) | 20 (18–22) (n = 70) |
| SW48 (hTDO) | < 20% inhibition @ 31,600 (n = 19) | 6,460 (5,650–7,390) (n = 24) |
| hWB + IFNγ (hIDO1) | 378 (349–408) (n = 12) | 54 (48–62) (n = 12) |
| mIDO1 | 93 (n = 2) | 39 (30–49) (n = 4) |
| mTDO | < 20% inhibition @ 31,600 (n = 2) | 225 (102–492) (n = 3) |
| B16F10-mIDO1 | 18 (n = 2) | 88 (n = 2) |
| GL-261-mTDO | < 20% inhibition @ 31,600 (n = 2) | 28% inhibition @ 31,600 (n = 2) |
Potency (IC50) in nM of IDO1 inhibitors NTRC 3883-0 and epacadostat in biochemical and cell-based assays for human (h) and mouse (m) IDO1 or TDO. 95% confidence intervals and number of experimental replicates (n) are given within brackets. hWB, human whole blood.