Product Details
| Product Name:
MSC2530818 |
CAS No.:
1883423-59-3 |
| Purity:
99.33% |
Supply Ability:
10g |
| Release date:
2024/11/19 |
Product Introduction
Bioactivity
| Name | MSC2530818 |
| Description | MSC2530818 is an effective, selective and orally available CDK8 inhibitor (IC50: 2.6 nM). |
| Animal Research | 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]. |
| In vitro | MSC2530818 binds to CDK8 and CDK19 with a similar affinity (4 nM) and shows potent inhibition of phospho-STAT1SER727, a biomarker of CDK8 activity, in SW620 human colorectal carcinoma cells (pSTAT1SER727 IC50=8±2 nM). It also inhibits WNT-dependent transcription in human cancer cell lines with activated WNT signaling, including LS174T (β-catenin mutant, IC50=32±7 nM), COLO205 (APC mutant, IC50=9±1 nM), and WNT3a ligand-dependent reporter readout in PA-1 cells (IC50=52±30 nM). Moreover, MSC2530818 exhibits a low efflux ratio in Caco-2 cells and does not inhibit any cytochrome P450 subtypes. |
| In vivo | Treatment with MSC2530818 in mice carrying tumors resulted in a notable reduction of tumor growth, presenting T/C ratios of 49% and 57%. This compound was well accepted, showing no impact on the body weight of mice under a daily (qd) administration regimen, aside from controllable body weight loss. Additionally, its pharmacokinetic profile in humans indicates a low clearance (0.14 L/h/kg) and a small volume of distribution at steady-state (0.48 L/kg), leading to a brief estimated terminal half-life of 2.4 hours. Moreover, physiologically based pharmacokinetic simulations predict that MSC2530818 could achieve an oral bioavailability of at least 75% when administered up to a daily dose of 500 mg. |
| Storage | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice. |
| Solubility Information | DMSO : 120 mg/mL (352.1 mM)
|
| Keywords | Cyclin dependent kinase | MSC-2530818 | Inhibitor | CDK | MSC 2530818 | inhibit | MSC2530818 |
| Inhibitors Related | Ribociclib | Ro-3306 | GSK 3 Inhibitor IX | Rafoxanide | Palbociclib monohydrochloride | CASIN | Palbociclib | GW 441756 | Sodium Oxamate | Abemaciclib | Dinaciclib | Abemaciclib methanesulfonate |
| Related Compound Libraries | Anti-Pancreatic Cancer Compound Library | Bioactive Compound Library | Kinase Inhibitor Library | Anti-Breast Cancer Compound Library | Inhibitor Library | NO PAINS Compound Library | Orally Active Compound Library | Anti-Aging Compound Library | Bioactive Compounds Library Max | Cell Cycle Compound Library |
Company Profile Introduction
Target Molecule Corp. (TargetMol) is a global high-tech enterprise, headquartered in Boston, MA, specializing in chemical and biological research product and service to meet the research needs of global customers.
TargetMol has evolved into one of the biggest global compound library and small molecule suppliers and a customer based on 40+ countries. TargetMol offers over 80 types of compound libraries and a wide range of high-quality research chemicals including inhibitors, activator, natural compounds, peptides, inhibitory antibodies, and novel life-science kits, for laboratory and scientific use. Besides, virtual screening service is also available for customers who would like to conduct the computer-aided drug discovery.
You may like
-
CAS:116285-77-9
$0.00 / 5mg
-
-
CAS:58442-64-1
$30.00 / 5mg
Recommended supplier
| Product name |
Price |
|
Suppliers |
Update time |
|
|
$/ |
|
Anhui Ruihan Technology Co., Ltd
|
2023-08-21 |
United States