MSC2530818
规格
| Cas Number | 1883423-59-3 |
| 规格或纯度 | ≥98% |
| 纯度 | ≥98% |
| 包装 | 100mg 或 50mg 或 10mg 或 1mg 或 5mg 或 25mg |
产品信息
| 品牌 | 阿拉丁 |
| 溶解性 | Solubility (25°C) In vitro DMSO: 68 mg/mL (199.52 mM); Ethanol: 68 mg/mL (199.52 mM); Water: Insoluble; |
| 简短描述 | CDK抑制剂 |
| 英文简短描述 | CDK Inhibitors |
| 过滤标签 | CDK,Cell Cycle/DNA Damage |
| 储存温度 | -20°C储存 |
| 运输条件 | 超低温冰袋运输 |
| 生化和生理学机理 | MSC2530818 是一种 IC50 值为 2.6 nM 的 CDK8 抑制剂，具有出色的激酶选择性、生化和细胞效力、微粒体稳定性和口服生物利用度。 |
| 英文描述 |
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-STAT1SER727 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. |