MCE 的所有產(chǎn)品僅用作科學(xué)研究或藥證申報，我們不為任何個人用途提供產(chǎn)品和服務(wù)。

MSC2530818

產(chǎn)品活性：MSC2530818是有效，選擇性，有口服活性的 CDK8 抑制劑，抑制 CDK8 的IC₅₀值為2.6 nM。

研究領(lǐng)域：Cell Cycle/DNA Damage

作用靶點：CDK

In Vitro: MSC2530818 binds to CDK8 and CDK19 with similar affinity (4 nM). Potent inhibition of phospho-STAT1^SER727, an established biomarker of CDK8 activity, in SW620 human colorectal carcinoma cells is also observed (pSTAT1^SER727 IC₅₀=8±2 nM). MSC2530818 demonstrates potent inhibition of WNT-dependent transcription in human cancer cell lines that have constitutively activated WNT signaling. For example, MSC2530818 inhibits the reporter-based luciferase readout in several cell lines bearing activating WNT-pathway mutations; LS174T (β-catenin mutant, IC₅₀=32±7 nM), COLO205 (APC mutant, IC₅₀=9±1 nM) and demonstrates inhibition of WNT3a ligand-dependent reporter readout in PA-1 cells (IC₅₀=52±30 nM). MSC2530818 demonstrates minimal activity in the CEREP panel, and demonstrates minimal hERG inhibition. Furthermore, MSC2530818 is a soluble CDK8 inhibitor with high permeability and low efflux ratio in Caco-2 cells and does not inhibit any cytochrome P450 subtypes.

In Vivo: Tumor-bearing mice treated with MSC2530818 shows reduction in tumor growth with T/C ratios (based on final tumor weights) of 49% and 57%, respectively. MSC2530818 is generally well tolerated, with no effects on mouse body weight in the qd administration schedule and manageable body weight loss. The human clearance and volume of distribution at steady-state are estimated to be low (0.14 L/h/kg) and small (0.48 L/kg), respectively, resulting in a short predicted terminal half-life (2.4 h). Physiologically based pharmacokinetics simulations suggested that human oral bioavailability may be ≥75% up to dose level of 500 mg daily.

相關(guān)產(chǎn)品：Bioactive Compound Library Plus  |  Cell Cycle/DNA Damage Compound Library  |  Kinase Inhibitor Library  |  Anti-Cancer Compound Library  |  Anti-Aging Compound Library  |  Orally Active Compound Library  |  Anti-Breast Cancer Compound Library  |  Anti-Blood Cancer Compound Library  |  Targeted Diversity Library  |  Cancer Stem Cells Compound Library  |  Heterocyclic Compound Library  |  Membrane Protein-targeted Compound Library  |  SY-5609  |  CLK1/2-IN-1  |  SB-218078  |  Toyocamycin  |  (S)-LY3177833 hydrate  |  Dinaciclib  |  EGFR/HER2/CDK9-IN-2  |  CDK8-IN-11  |  SNS-032  |  M2N12  |  Palbociclib-d₈  |  EGFR/CDK2-IN-1  |  BSJ-04-132  |  (E/Z)-Zotiraciclib  |  CCT-251921  |  BS-181  |  Ribociclib-d₈  |  CDK9-IN-9  |  Flavopiridol  |  SRI-29329  |  dCeMM4  |  GSK 3 Inhibitor IX  |  CDK9-IN-7  |  BSJ-03-204  |  Amantadine-d₆  |  K00546  |  Abemaciclib metabolite M18 hydrochloride  |  Ribociclib-d₆  |  Lacto-N-fucopentaose I  |  CDK2/4/6-IN-2

品牌介紹:
•   MCE (MedChemExpress) 擁有200 多種*僅有化合物庫，我們致力于為*科研客戶提供前沿的高品質(zhì)小分子活性化合物；
•   50,000 多種高選擇性抑制劑、激動劑涉及各熱門信號通路及疾病領(lǐng)；
•   產(chǎn)品種類涵蓋各種重組蛋白，多肽，常用試劑盒 ，更有 PROTAC、ADC 等特色產(chǎn)品，廣泛應(yīng)用于新藥研發(fā)、生命科學(xué)等科研項目；
•   提供虛擬篩選，離子通道篩選，代謝組學(xué)分析檢測分析，藥物篩選等專業(yè)技術(shù)服務(wù)；
•   設(shè)有專業(yè)的實驗中心和嚴(yán)格的質(zhì)控、驗證體系；
•   提供 LC/MS、NMR、HPLC、手性分析、元素分析等各項質(zhì)檢報告，確保產(chǎn)品的高純度、高品質(zhì)；
•   產(chǎn)品的生物活性多經(jīng)各國客戶實驗驗證；
•   Nature, Cell, Science 等多種頂級期刊及制藥 Patent 收錄了MCE客戶的科研成果；
•   專業(yè)團(tuán)隊跟蹤新的制藥及生命科學(xué)研究進(jìn)展，為您提供*新的活性化合物；
•   與世界各大制藥公司及*科研機(jī)構(gòu)建立了長期的合作。