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CDK8-IN-11
本产品不向个人销售,仅用作科学研究,不用于任何人体实验及非科研性质的动物实验。
CDK8-IN-11图片
包装与价格:
包装价格(元)
100mg电议
250mg电议
500mg电议

产品介绍
CDK8-IN-11 是一种有效的、选择性的CDK8抑制剂,IC50值为 46 nM。CDK8-IN-11 可抑制 WNT/β-catenin 信号通路。CDK8-IN-11 可用于结肠癌的研究。
生物活性

CDK8-IN-11 is a potent and selectiveCDK8inhibitor with anIC50value of 46 nM. CDK8-IN-11 inhibits WNT/β-catenin signaling pathway. CDK8-IN-11 can be used in the research of coloncancer[1].

IC50& Target[1]

CDK8

46 nM (IC50)

体外研究
(In Vitro)

CDK8-IN-11 (compound 29, 200 nM) shows inhibitory effects against CDK8 by 73.6%[1].
CDK8-IN-11 (0-50 μM, 48 h) inhibits cell proliferation in HCT-116, HHT-29, SW480, CT-26, GES-1 cells[1].
CDK8-IN-11 (0-4 μM, 48 h) inhibits the phosphorylation of STAT1 at Ser727 mediated by CDK8 in HCT-116 cells[1].
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[1].
CDK8-IN-11 (0.5-2 μM, 48 h) increases the number of cells in the G1 phase in HCT-116 cells[1].
CDK8-IN-11 (0-4 μM) reversesSorafenib(HY-10201) resistance of HCT-116 cells[1].

Cell Proliferation Assay[1]

Cell Line:HCT-116, HHT-29, SW480, CT-26, GES-1 cells
Concentration:0.08, 0.4, 2, 10, and 50 μM
Incubation Time:48 h
Result:Inhibited cell proliferation with IC50values of 1.2, 0.7, 2.4, 5.5, 62.7 nM respectively.

Western Blot Analysis[1]

Cell Line:HCT-116 cell
Concentration:0, 1, 2, 4 μM
Incubation Time:48 h
Result:Inhibited the phosphorylation of STAT1 at Ser727 without affecting the JAK-regulated phosphorylation at Tyr701.

Cell Cycle Analysis[1]

Cell Line:HCT-116 cell
Concentration:0.5-2 μM
Incubation Time:48 h
Result:Increased the number of cells in the G1 phase with an obvious decreased percentage of cells in the G2/M and S phase in HCT-116 cells.
体内研究
(In Vivo)

CDK8-IN-11 (compound 29, 10 and 40 mg/kg, p.o.) inhibits tumor growth in CT-26 xenograft mice[1].
CDK8-IN-11 (1000 mg/kg, oral gavage, ICR mice) shows no obvious abnormal behavior within 7 days[1].
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 × 10–6cm/s[1].

Animal Model:CT-26 xenograft mice[1]
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)[1]
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.)1.10.845331.7
2 (i.v.)0.5318
分子量

388.34

Formula

C19H15F3N4O2

运输条件

Room temperature in continental US; may vary elsewhere.

储存方式

Please store the product under the recommended conditions in the Certificate of Analysis.