化合物 MSC2530818|TQ0266|TargetMol

MSC2530818
1883423-59-3

￥461 1mg 起订

￥1160 5mg 起订

￥1870 10mg 起订

上海更新日期：2024-12-12

TargetMol中国（陶术生物）

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联系人：邵小姐

手机：4008200310 拨打

邮箱：marketing@tsbiochem.com

产品详情:

中文名称：: 化合物 MSC2530818

英文名称：: MSC2530818

CAS号：: 1883423-59-3

品牌：: TargetMol

产地：: 美国

保存条件：: Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice.

纯度规格：: 99.33%

产品类别：: 抑制剂

货号：: TQ0266

Product Introduction

Bioactivity

名称	MSC2530818
描述	MSC2530818 is an effective, selective and orally available CDK8 inhibitor (IC50: 2.6 nM).
动物实验	MSC2530818 is assessed in an established SW620 human colorectal cancer xenograft model in female NCr athymic mice. Tumor-bearing mice are treated orally with MSC2530818 (50 mg/kg bid or 100 mg/kg qd) for 16 days. Tumor weights are measured and body weights are monitored [1].
体外活性	MSC2530818 binds to CDK8 and CDK19 with a similar affinity (4 nM). Potent inhibition of phospho-STAT1SER727, an established biomarker of CDK8 activity, in SW620 human colorectal carcinoma cells is also observed (pSTAT1SER727 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). Furthermore, MSC2530818 is a low efflux ratio in Caco-2 cells and does not inhibit any cytochrome P450 subtypes.
体内活性	Tumor-bearing mice treated with MSC2530818 shows a 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 maybe ≥75% up to a dose level of 500 mg daily.
存储条件	Powder: -20°C for 3 years \| In solvent: -80°C for 1 year \| Shipping with blue ice.
溶解度	DMSO : 120 mg/mL (352.1 mM)
关键字	Cyclin dependent kinase \| MSC-2530818 \| Inhibitor \| CDK \| MSC 2530818 \| inhibit \| MSC2530818
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相关库	抑制剂库 \| 经典已知活性库 \| 抗癌化合物库 \| 已知活性化合物库 \| 细胞周期化合物库 \| 抗胰腺癌化合物库 \| 激酶抑制剂库 \| 抗衰老化合物库 \| NO PAINS 化合物库 \| 口服活性化合物库

MSC2530818|TargetMol

TargetMol Chemicals Inc. 总部位于马萨诸塞州波士顿，致力于为全球生化领域科学家的研究提供专业的产品和服务。TargetMol?品牌的客户群分布于40多个国家和地区，已发展成为全球知名的化合物库和小分子化合物研究供应商。 TargetMol?可提供160多种满足不同需求的化合物库，以及多种类型的生化试剂产品，包括12000多种抑制剂、16000多种天然产物和各类多肽、抗体、生命科学试剂盒等，此外，我们还建设有CADD（计算机辅助药物设计）研究中心、药理实验室、药化合成平台三大技术中心，全方位满足客户的定制需求。凭借我们优质的产品和服务、快速高效的全球供应链和专业的技术支持，我们将有效帮助您缩短研发周期，取得更成功的结果。

成立日期	(12年)
注册资本	566.265100万人民币
员工人数	100-500人
年营业额	￥ 1亿以上
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主营行业	天然产物,生化试剂,分子生物学,分子砌块,生物技术服务