SHR0302 是一种具有口服活性的JAK抑制剂。它对JAK1的结合力是JAK2的 10 倍以上，是JAK3的 77 倍，是Tyk2的 420 倍。它抑制JAK1-STAT3磷酸化并诱导肝星状细胞凋亡，具有抗增殖和抗炎作用。

SHR0302 is a JAK inhibitor that binds JAK1 with stronger affinity than others (Selectivity for JAK1 is more than 10 times for JAK2, 77 times for JAK3, 420 times for Tyk2).

SHR0302 (1nM-10μM) exerted an inhibitory effect on the activation, proliferation and migration of hepatic stellate cells (HSCs). SHR0302 induced the apoptosis of HSCs. The pharmacological inhibition of the JAK1/signal transducer and activator of transcription (STAT)3 pathway led to the disruption of functions essential for HSC[1].

SHR0302 may attenuate the severity of AA rats, partially through reducing Th17 function and total B cell proportion by inhibiting JAK1-STAT3 phosphorylation[2].

1445987-21-2

C18H22N8O2S

414.49

ARQ252

DMSO:30mg/ml(72.38mM),Need ultrasonic
Powder: -20°C for 3 years
In solvent: -80°C for 2 years