产品
编 号：F756292
分子式：C19H15F3N4O2
分子量：388.34
分子式：C19H15F3N4O2
分子量：388.34
产品类型
规格
价格
是否有货
5mg
询价
询价
10mg
询价
询价
25mg
询价
询价
50mg
询价
询价
结构图
CAS No: 2839338-28-0
产品详情
生物活性：
CDK8-IN-11 is a potent and selective CDK8 inhibitor with an IC50 value of 46 nM. CDK8-IN-11 inhibits WNT/β-catenin signaling pathway. CDK8-IN-11 can be used in the research of colon cancer.
体内研究：
CDK8-IN-11 (compound 29, 10 and 40 mg/kg, p.o.) inhibits tumor growth in CT-26 xenograft mice.CDK8-IN-11 (1000 mg/kg, oral gavage, ICR mice) shows no obvious abnormal behavior within 7 days.CDK8-IN-11 (10 mg/kg, p.o.; 2 mg/kg, i.v., rats) shows moderate permeability with an apparent permeability coefficient value of 1.8 × 10?6 cm/s.Animal Model:CT-26 xenograft mice
Dosage:10 and 40 mg/kg
Administration:Oral adminstration (p.o.)
Result:Reduced the tumor volume, reduced β-catenin and c-Myc level in tumor.
Animal Model:Rats (pharmacokinetic assay)
Dosage:10 mg/kg (p.o.), 2 mg/kg (i.v.)
Administration:Oral adminstration (p.o.) or intravenous injection (i.v.)
Result:Pharmacokinetic profile of CDK8-IN-11 (compound 29). dose (mg/kg)T1/2 (h) Tmax (h)Cmax (ng/mL)F (%)
10 (p.o.)1.10.8453 31.7
2 (i.v.)0.5 318
体外研究：
CDK8-IN-11 (compound 29, 200 nM) shows inhibitory effects against CDK8 by 73.6% .CDK8-IN-11 (0-50 μM, 48 h) inhibits cell proliferation in HCT-116, HHT-29, SW480, CT-26, GES-1 cells.CDK8-IN-11 (0-4 μM, 48 h) inhibits the phosphorylation of STAT1 at Ser727 mediated by CDK8 in HCT-116 cells.CDK8-IN-11 (0-4 μM, 24 h) suppresses canonical WNT/β-catenin signaling pathways and deregulates β-catenin-mediated transcription in HCT-116 cells.CDK8-IN-11 (0.5-2 μM, 48 h) increases the number of cells in the G1 phase in HCT-116 cells.CDK8-IN-11 (0-4 μM) reverses Sorafenib (HY-10201) resistance of HCT-116 cells.
CDK8-IN-11 is a potent and selective CDK8 inhibitor with an IC50 value of 46 nM. CDK8-IN-11 inhibits WNT/β-catenin signaling pathway. CDK8-IN-11 can be used in the research of colon cancer.
体内研究：
CDK8-IN-11 (compound 29, 10 and 40 mg/kg, p.o.) inhibits tumor growth in CT-26 xenograft mice.CDK8-IN-11 (1000 mg/kg, oral gavage, ICR mice) shows no obvious abnormal behavior within 7 days.CDK8-IN-11 (10 mg/kg, p.o.; 2 mg/kg, i.v., rats) shows moderate permeability with an apparent permeability coefficient value of 1.8 × 10?6 cm/s.Animal Model:CT-26 xenograft mice
Dosage:10 and 40 mg/kg
Administration:Oral adminstration (p.o.)
Result:Reduced the tumor volume, reduced β-catenin and c-Myc level in tumor.
Animal Model:Rats (pharmacokinetic assay)
Dosage:10 mg/kg (p.o.), 2 mg/kg (i.v.)
Administration:Oral adminstration (p.o.) or intravenous injection (i.v.)
Result:Pharmacokinetic profile of CDK8-IN-11 (compound 29). dose (mg/kg)T1/2 (h) Tmax (h)Cmax (ng/mL)F (%)
10 (p.o.)1.10.8453 31.7
2 (i.v.)0.5 318
体外研究：
CDK8-IN-11 (compound 29, 200 nM) shows inhibitory effects against CDK8 by 73.6% .CDK8-IN-11 (0-50 μM, 48 h) inhibits cell proliferation in HCT-116, HHT-29, SW480, CT-26, GES-1 cells.CDK8-IN-11 (0-4 μM, 48 h) inhibits the phosphorylation of STAT1 at Ser727 mediated by CDK8 in HCT-116 cells.CDK8-IN-11 (0-4 μM, 24 h) suppresses canonical WNT/β-catenin signaling pathways and deregulates β-catenin-mediated transcription in HCT-116 cells.CDK8-IN-11 (0.5-2 μM, 48 h) increases the number of cells in the G1 phase in HCT-116 cells.CDK8-IN-11 (0-4 μM) reverses Sorafenib (HY-10201) resistance of HCT-116 cells.
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