BMS-986165

Description:Tyk2-IN-4 is a selective, potent, allosteric inhibitor of tyrosine kinase 2 (Tyk2).

Target:Tyk2

In Vitro:Tyk2-IN-4 blocks receptor-mediated Tyk2 activation by stabilizing the regulatory pseudokinase domain of the protein.

In Vivo:Lupus-like disease is strongly inhibited in NZB/W mice treated with Tyk2-IN-4. Tyk2-IN-4 is safe and overall well-tolerated. There are no serious adverse events and the frequency of non-serious adverse events are similar in the active (75%) and placebo (76%) groups. After oral administration, Tyk2-IN-4 is rapidly absorbed and exhibits an apparent elimination half-life of 8-15 hours.

Molecular Formula：C20H19D3N8O3

Molecular Weight：425.46