SHR0302 是一种有效的具有口服活性的 JAK 抑制剂，尤其是 JAK1 的抑制剂。SHR0302 对 JAK1 的选择性是 JAK2 的 10 倍以上，是 JAK3 的 77 倍，是 Tyk2 的 420 倍。SHR0302 抑制 JAK1-STAT3 磷酸化并诱导肝星状细胞凋亡 (apoptosis)。SHR0302 具有抗增殖和抗炎作用。
SHR0302 is a potent and orally active all members of the JAK family inhibitor, particularly JAK1. The selectivity of SHR0302 for JAK1 is >10-fold for JAK2, 77-fold for JAK3, 420-fold for Tyk2. SHR0302 inhibits JAK1-STAT3 phosphorylation and induces the apoptosis of hepatic stellate cells. SHR0302 has anti-proliferative and anti-inflammatory effects[1][2].
[1]. Huaxun Wu, et al. JAK1-STAT3 Blockade by JAK Inhibitor SHR0302 Attenuates Inflammatory Responses of Adjuvant-Induced Arthritis Rats and Decreases Th17 and Total B Cells. Joint Bone Spine. 2016 Oct;83(5):525-32. [2]. Yuan-Jing Gu, et al. Targeted Blockade of JAK/STAT3 Signaling Inhibits Proliferation, Migration and Collagen Production as Well as Inducing the Apoptosis of Hepatic Stellate Cells. Int J Mol Med. 2016 Sep;38(3):903-11.
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