aladdin 阿拉丁 M413996 MSC2530818 1883423-59-3 98%

中文名：MSC2530818

英文名：MSC2530818

纯度：≥98%

货号：M413996

Cas号：1883423-59-3

存储温度：-20°C储存

运输条件：超低温运输

产品介绍：

Information

MSC2530818 MSC2530818, a CDK8 inhibitor with the IC50 of 2.6 nM, displays excellent kinase selectivity, biochemical and cellular potency, microsomal stability, and is orally bioavailable.

Targets

CDK8 (Cell-free assay) 2.6 nM

In vitro

MSC2530818 binds to CDK8 and CDK19 with similar affinity (4 nM) and shows potent inhibition of phospho-STAT1^SER727 in SW620 human colorectal carcinoma cells (IC50=8 ± 2 nM). It also demonstrates potent inhibition of WNT-dependent transcription in human cancer cell lines that have constitutively activated WNT signaling. MSC2530818 is a soluble CDK8 inhibitor with high permeability and low efflux ratio in Caco-2 cells (ER = 1.5) and does not inhibit any cytochrome P450 subtypes (Cyp IC50s > 20 μM).

In vivo

MSC2530818 shows acceptable pharmacokinetics (PK) in all tested preclinical species (mouse, rat, dog). It demonstrates reduction of tumor growth rates of established human SW620 colorectal carcinoma xenografts.

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