SHR-0302

SHR-0302 is a JAK inhibitor (IC50s = 0. 0. and 7. nM for JAK1, -2, and -3, respectively). It is selective for these kinases over tyrosine kinase 2 (TYK2, IC50 = 42 nM). SHR-0302 inhibits the activation, proliferation, and TGF-beta-1-induced migration of HSC-T6 rat hepatic stellate cells when used at concentrations ranging from 0. to 10 µM. It also decreases collagen production and JAK1 and STAT3 phosphorylation in HSC-T6 cells. In vivo, SHR-0302 (3 mg/kg) decreases disease severity and paw swelling in a rat model of adjuvant-induced arthritis. It increases survival, white blood cell count, red blood cell count, and platelet count and decreases body weight loss and disease severity in a mouse model of bone marrow transplant-induced graft-versus-host disease (GVHD) when administered prophylactically at a dose of 5 mg/kg.. Solulibility: DMSO: Sparingly Soluble: 1-10 mg/ml: .