产品
编 号：F274376
分子式：C22H20N4O
分子量：356.42
分子式：C22H20N4O
分子量：356.42
产品类型
规格
价格
是否有货
10mM*1mL in DMSO
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1mg
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5mg
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10mg
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50mg
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100mg
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结构图
CAS No: 2163056-91-3
产品详情
生物活性：
BI-1347 is an orally active, selective and potent CDK8 inhibitor (IC50=1.1 nM). BI-1347 shows anti-tumoral activity.
体内研究：
BI-1347 (oral gavage; 10 mg/kg; once daily; 30 d) modulates STAT1 S727 phosphorylation and shows anti-tumor activity in vivo.BI-1347 (oral gavage; 10 mg/kg) intermittent schedule and BI-8382 continuous treatment combination treatment increases efficacy compared to each monotherapy in the mammary carcinoma EMT6 model.Animal Model:B16-F10-luc2 syngeneic melanoma model
Dosage:10 mg/kg
Administration:Oral gavage; 10 mg/kg; once daily; 30 d
Result:Reduced phosphorylation of STAT1 S727 for at least 6 h by 60%.Showed minimal effect on body weight at 10 mg/kg.Showed lower tumor burden both on day 23 and 29, compared to the control group.
体外研究：
BI-1347 (150 nM; 44 h) enhances granzyme B (GZMB+) production in mouse splenic NK cells.BI-1347 (0.1 nM-10 μM; 24 h) treatment increases perforin secretion from NK92MI cells.
BI-1347 is an orally active, selective and potent CDK8 inhibitor (IC50=1.1 nM). BI-1347 shows anti-tumoral activity.
体内研究：
BI-1347 (oral gavage; 10 mg/kg; once daily; 30 d) modulates STAT1 S727 phosphorylation and shows anti-tumor activity in vivo.BI-1347 (oral gavage; 10 mg/kg) intermittent schedule and BI-8382 continuous treatment combination treatment increases efficacy compared to each monotherapy in the mammary carcinoma EMT6 model.Animal Model:B16-F10-luc2 syngeneic melanoma model
Dosage:10 mg/kg
Administration:Oral gavage; 10 mg/kg; once daily; 30 d
Result:Reduced phosphorylation of STAT1 S727 for at least 6 h by 60%.Showed minimal effect on body weight at 10 mg/kg.Showed lower tumor burden both on day 23 and 29, compared to the control group.
体外研究：
BI-1347 (150 nM; 44 h) enhances granzyme B (GZMB+) production in mouse splenic NK cells.BI-1347 (0.1 nM-10 μM; 24 h) treatment increases perforin secretion from NK92MI cells.
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