Table 3.
Cellular Potency of RB1 in Total Lymphocytes in Human Peripheral Blood Mononuclear Cellsa.
JAKs Involved | Trigger | Readout | IC5044 | Selectivity | ||
---|---|---|---|---|---|---|
JAK1/JAK3 or JAK2/JAK3 | ||||||
RB1 | Tofacitinib | RB1 | Tofacitinib | |||
JAK1/JAK3 | IL-2 | pSTAT5 | 105 | 30 | — | — |
JAK1 | IL-6 | pSTAT3 | >40000 | 73 | >400 | 2.4 |
JAK2 | GM-CSF | pSTAT5 | >10000 | 659 | >100 | 22 |
aRB1 cellular IC50 values for the phosphorylation of STAT proteins in response to various cytokine treatments.