BMS-986202

Biorbyt

BMS-986202

10

1771691-34-9

Research Use Only

C22H21FN6O3

439.4574

BMS-986202 (BMS 986202) is potent, selective Tyk2 inhibitor that binds to Tyk2 JH2 domain with IC50 of 0.19 nM, Ki of 0.02 nM, > 10,000-fold over 273 kinases and pseudokinases; BMS-986202 demonstrated cellular activity (IL-23 IC50=12 nM) in IL-23 stimulated reporter assay (in Kit225 T cells). BMS-986202 also binds Jak1 JH2 with an IC50 of 7.8 nM, but this enzymatic binding did not lead to any functional activities, as BMS-986202 displayed an activity (IC50) of greater than 12.5 microM in the IL-2 stimulated Jak1/3-dependent cellular assay. BMS-986202 showed in vivo efficacy in mouse models of IL-23-driven acanthosis, anti-CD40-induced colitis, and spontaneous lupus.

FC1C([H])=NC(C2C([H])=C([H])C([H])=C(C=2OC([H])([H])[H])N([H])C2C(C(N([H])C([2H])([2H])[2H])=O)=C([H])N=C(C=2[H])N([H])C(C2([H])C([H])([H])C2([H])[H])=O)=NC=1[H]

12352200