Golidocitinib,2091134-68-6

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Golidocitinib

CAS No. : 2091134-68-6

MCE 国际站：Golidocitinib

产品活性：Golidocitinib (AZD4205) 是一种选择性的 JAK1 抑制剂，IC₅₀ 值为 73 nM，对 JAK2 的抑制作用较弱 (IC₅₀>14.7 μM)，对 JAK3 的抑制作用很小 (IC₅₀>30 μM)。

研究领域：Epigenetics  |  Protein Tyrosine Kinase/RTK  |  JAK/STAT Signaling  |  Stem Cell/Wnt

作用靶点：JAK

In Vitro: Golidocitinib (Example 32) is a selective JAK1 inhibitor, with an IC₅₀ of 73 nM, weakly inhibits JAK2, and shows little inhibition on JAK3 (IC₅₀, >14.7, >30 μM, respectively). Golidocitinib significantly inhibits STAT3 phosphorylation in NCI-H 1975 cells with an IC₅₀ of 161 nM.

In Vivo: Golidocitinib (12.5 mg/kg BID (twice daily), 25 m/kg BID or 50 mg/kg BID, p.o.) alone has increasing antitumor effects, and ehances the antitumor activity of osimertinib, compared to treatment with osimertinib alone in mice bearing NCI-H1975 cells.

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