产品
编 号：F741673
分子式：C26H33N7O
分子量：459.59
分子式：C26H33N7O
分子量：459.59
产品类型
规格
价格
是否有货
10mM*1mL in DMSO
询价
询价
1mg
询价
询价
5mg
询价
询价
10mg
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询价
结构图
CAS No: 2593402-36-7
产品详情
生物活性：
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.
体内研究：
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.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.Animal Model:SET-2 cell-inoculated xenograft NOD/SCID mouse model
Dosage:15, 30, and 60 mg/kg
Administration:Orally daily for 16 days
Result:Exhibited a significant tumor growth inhibition of 82.3% without obvious weight change.
体外研究：
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.JAK2-IN-7 (10-160 nM; 24 hours) induces cell arrest in the G0/G1 phase.JAK2-IN-7 (0.05-1.6 μM; 2 hours) induces apoptosis in SET-2 cells.
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.
体内研究：
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.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.Animal Model:SET-2 cell-inoculated xenograft NOD/SCID mouse model
Dosage:15, 30, and 60 mg/kg
Administration:Orally daily for 16 days
Result:Exhibited a significant tumor growth inhibition of 82.3% without obvious weight change.
体外研究：
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.JAK2-IN-7 (10-160 nM; 24 hours) induces cell arrest in the G0/G1 phase.JAK2-IN-7 (0.05-1.6 μM; 2 hours) induces apoptosis in SET-2 cells.
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