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MSC2530818

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Chemical Structure| 1883423-59-3 同义名 : -
CAS号 : 1883423-59-3
货号 : A291701
分子式 : C18H17ClN4O
纯度 : 99%+
分子量 : 340.807
MDL号 : MFCD31382190
存储条件：

粉末 Sealed in dry,2-8°C

液体 -20°C:3-6个月-80°C:12个月
溶解度 :

DMSO: 105 mg/mL(308.09 mM)，配合低频超声助溶，注意：DMSO长时间开封后，会吸水并导致溶解能力下降，请避免使用长期开封的DMSO
动物实验配方：
生物活性
靶点

  • CDK8

    CDK8, IC50:2.6 nM
描述 MSC2530818 binds to CDK8 and CDK19 with similar affinity (IC50 of 4 nM). It effectively inhibits the phosphorylation of STAT1SER727 (a biomarker of CDK8 activity) in SW620 human colorectal cancer cells (pSTAT1SER727 IC50=8±2 nM). MSC2530818 shows effective inhibition of WNT-dependent transcription in human cancer cell lines with constitutively active WNT signaling. For instance, MSC2530818 inhibits luciferase readings from reporter genes in several cell lines with mutations activating the WNT pathway; LS174T (β-catenin mutant, IC50=32±7 nM), COLO205 (APC mutant, IC50=9±1 nM) and shows inhibition of WNT3a ligand-dependent reporter gene readings in PA-1 cells (IC50=52±30 nM). MSC2530818 exhibits minimal activity in the CEREP panel and minimal hERG inhibition. Additionally, MSC2530818 is a soluble CDK8 inhibitor with high permeability and low efflux in Caco-2 cells, and does not inhibit any cytochrome P450 subtypes[1].
实验方案
1mg 5mg 10mg

1 mM

5 mM

10 mM

2.93mL

0.59mL

0.29mL

14.67mL

2.93mL

1.47mL

29.34mL

5.87mL

2.93mL
参考文献

[1]Czodrowski P, et al. Structure-Based Optimization of Potent, Selective, and Orally Bioavailable CDK8 Inhibitors Discovered by High-Throughput Screening. J Med Chem. 2016 Oct 27;59(20):9337-9349.