JAK1-IN-3是一种选择性的JAK1抑制剂，IC50值为73nM，对JAK2的抑制作用较弱，对JAK3的抑制作用很小，IC50值分别为>14.7，>30μM。
货号:ajcx12866
CAS:2091134-68-6
分子式:C25H31N9O2
分子量：489.57
溶解度:DMSO: 250 mg/mL (510.65 mM)
纯度：98%
存储：Store at -20°C
库存：现货

Background:

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.