产品
编 号：F199402
分子式：C23H24ClN5O
分子量：421.92
分子式：C23H24ClN5O
分子量：421.92
产品类型
规格
价格
是否有货
10mM*1mL in DMSO
询价
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2mg
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5mg
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10mg
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25mg
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50mg
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结构图
CAS No: 1661839-45-7
产品详情
生物活性：
CCT251545 is an orally bioavailable and potent inhibitor of WNT signaling with an IC50 of 5 nM in 7dF3 cells. CCT251545 is a selective chemical probe for exploring the role of CDK8 and CDK19 in human disease.
体内研究：
CCT251545 (70mg/kg; p.o.; twice daily) causes an inhibition of tumor growth in NCr athymic mice bearing established SW620 human colorectal cancer xenografts.Animal Model:6-8 weeks female NCr athymic mice bearing established SW620 xenografts
Dosage:70mg/kg
Administration:Oral administration; twice daily; from days 0-7 and days 10-14
Result:Caused an inhibition of tumor growth with a 70% reduction in final tumor weight relative to control.
体外研究：
CCT251545 potently inhibits WNT pathway activity in COLO205-F1756 clone 4 (an APC -mutant human colorectal cancer cell line engineered to express a modified luciferase-based WNT reporter construct) with an IC50 of 0.035 μM.CCT251545 has weak inhibition of tankyrase enzymes (TNKS1 IC50 > 10 μM, TNKS2 IC50 = 15.0).CCT251545 is a potent and selective chemical probe for the human mediator complex-associated protein kinases CDK8 and CDK19 with >100-fold selectivity over 291 other kinases.CCT251545 alters WNT pathway-regulated gene expression and other on-target effects of modulating CDK8 and CDK19, including expression of genes regulated by STAT1.CCT251545 also reduces phospho-STAT1SER727 levels in SW620 cells with an IC50 of 9 nM.CCT251545 displays potent cell-based activity.
CCT251545 is an orally bioavailable and potent inhibitor of WNT signaling with an IC50 of 5 nM in 7dF3 cells. CCT251545 is a selective chemical probe for exploring the role of CDK8 and CDK19 in human disease.
体内研究：
CCT251545 (70mg/kg; p.o.; twice daily) causes an inhibition of tumor growth in NCr athymic mice bearing established SW620 human colorectal cancer xenografts.Animal Model:6-8 weeks female NCr athymic mice bearing established SW620 xenografts
Dosage:70mg/kg
Administration:Oral administration; twice daily; from days 0-7 and days 10-14
Result:Caused an inhibition of tumor growth with a 70% reduction in final tumor weight relative to control.
体外研究：
CCT251545 potently inhibits WNT pathway activity in COLO205-F1756 clone 4 (an APC -mutant human colorectal cancer cell line engineered to express a modified luciferase-based WNT reporter construct) with an IC50 of 0.035 μM.CCT251545 has weak inhibition of tankyrase enzymes (TNKS1 IC50 > 10 μM, TNKS2 IC50 = 15.0).CCT251545 is a potent and selective chemical probe for the human mediator complex-associated protein kinases CDK8 and CDK19 with >100-fold selectivity over 291 other kinases.CCT251545 alters WNT pathway-regulated gene expression and other on-target effects of modulating CDK8 and CDK19, including expression of genes regulated by STAT1.CCT251545 also reduces phospho-STAT1SER727 levels in SW620 cells with an IC50 of 9 nM.CCT251545 displays potent cell-based activity.
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