JAK2-IN-7 |
| Catalog No.GC62500 |
JAK2-IN-7은 JAK2, SET-2 및 Ba/F3V617F 세포에 대해 IC50이 각각 3, 11.7 및 41nM인 선택적 JAK2 억제제입니다. JAK2-IN-7은 JAK1, JAK3, FLT3에 비해 14배 이상의 선택성을 가지고 있습니다. JAK2-IN-7은 G0/G1 단계에서 세포 주기 정지를 자극하고 종양 세포자멸사를 유도합니다. 항종양 활동.
Products are for research use only. Not for human use. We do not sell to patients.
Cas No.: 2593402-36-7
Sample solution is provided at 25 µL, 10mM.
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JAK2-IN-7 is a selective JAK2 inhibitor with IC50s of 3, 11.7, and 41 nM for JAK2, SET-2, and Ba/F3V617F cells, respectively. JAK2-IN-7 possesses >14-fold selectivity over JAK1, JAK3, FLT3. JAK2-IN-7 stimulates cell cycle arrest in the G0/G1 phase and induces tumor cellapoptosis. Antitumor activities[1].
JAK2-IN-7 (compound 13ac) (0-1000 nM; 2 hours) inhibits JAK2 and STAT5 phosphorylation in a dose-dependent manner in SET-2 and Ba/F3-JAK2V617F cells[1].JAK2-IN-7 (10-160 nM; 24 hours) induces cell arrest in the G0/G1 phase[1].JAK2-IN-7 (0.05-1.6 μM; 2 hours) induces apoptosis in SET-2 cells[1].
JAK2-IN-7 (15-60 mg/kg; p.o.; daily for 16 days) shows potent in vivo antitumor efficacy with 82.3% tumor growth inhibition in the SET-2 xenograft model[1].JAK2-IN-7 (30-60 mg/kg; p.o.; q.d. for 16 day) significantly ameliorates the disease symptoms in a Ba/F3-JAK2V617F allograft model, with 77.1% normalization of spleen weight, which was more potent than Ruxolitinib[1].
[1]. Yang T, et al. N-(Pyrimidin-2-yl)-1,2,3,4-tetrahydroisoquinolin-6-amine Derivatives as Selective Janus Kinase 2 Inhibitors for the Treatment of Myeloproliferative Neoplasms [published online ahead of print, 2020 Nov 30]. J Med Chem. 2020;10.1021/acs.jmedchem.0c01488.
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