價格 | ¥11100 | ¥5930 | ¥7870 |
包裝 | 100mg | 25mg | 50mg |
最小起訂量 | 1mg |
發(fā)貨地 | 上海 |
更新日期 | 2025-05-20 |
中文名稱:化合物 CDK8-IN-11 | 英文名稱:CDK8-IN-11 |
CAS:2839338-28-0 | 品牌: TargetMol |
產(chǎn)地: 美國 | 保存條件: Shipping with blue ice. |
產(chǎn)品類別: 抑制劑 | |
貨號: T61742 |
Name | CDK8-IN-11 |
Description | CDK8-IN-11 is a potent and selective inhibitor of CDK8, demonstrating an IC50 of 46 nM, and effectively targets the WNT/β-catenin signaling pathway. This compound has potential applications in colon cancer research [1]. |
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) reverses Sorafenib 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 IC 50 values 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. |
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 6 cm/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) T 1/2 (h) T max (h) C max (ng/mL) F (%) 10 (p.o.) 1.1 0.8 453 31.7 2 (i.v.) 0.5 318 |
Storage | Shipping with blue ice. |
成立日期 | 2013-04-18 (13年) | 注冊資本 | 589.8595萬人民幣 |
員工人數(shù) | 100-500人 | 年營業(yè)額 | ¥ 1億以上 |
主營行業(yè) | 中間體,天然產(chǎn)物,生物化工,化學試劑,生物技術服務 | 經(jīng)營模式 | 貿(mào)易,工廠,試劑,定制,服務 |
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