JAK1-IN-3 (Synonyms: Golidocitinib; AZD4205) |
| رقم الكتالوجGC33036 |
JAK1-IN-3 (AZD4205) هو مثبط انتقائي JAK1 ، مع IC50 من 73 نانومتر ، يثبط بشكل ضعيف JAK2 (IC50> 14.7 μ ؛ M) ، ويظهر القليل من تثبيط JAK3 (IC50> 30 μ ؛ M).
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Cas No.: 2091134-68-6
Sample solution is provided at 25 µL, 10mM.
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JAK1-IN-3 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).
JAK1-IN-3 (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). JAK1-IN-3 significantly inhibits STAT3 phosphorylation in NCI-H 1975 cells with an IC50 of 161 nM[1].
JAK1-IN-3 (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[1].
[1]. Annika Birgitta Margareta ?STRAND, et al. Compounds and methods for inhibiting jak.
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