Powder: -20°C for 3 years | In solvent: -80°C for 1 year
MSC2530818 is an effective, selective and orally available CDK8 inhibitor (IC50: 2.6 nM).
Pack Size | Availability | Price/USD | Quantity |
---|---|---|---|
1 mg | In stock | $ 60.00 | |
5 mg | In stock | $ 147.00 | |
10 mg | In stock | $ 242.00 | |
25 mg | In stock | $ 535.00 | |
50 mg | In stock | $ 773.00 | |
100 mg | In stock | $ 1,080.00 | |
1 mL * 10 mM (in DMSO) | In stock | $ 162.00 |
Description | MSC2530818 is an effective, selective and orally available CDK8 inhibitor (IC50: 2.6 nM). |
Targets&IC50 | CDK8:2.6 nM (cell free) |
In vitro | 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. |
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. |
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]. |
Molecular Weight | 340.81 |
Formula | C18H17ClN4O |
CAS No. | 1883423-59-3 |
Powder: -20°C for 3 years | In solvent: -80°C for 1 year
DMSO: 120 mg/mL (352.1 mM)
You can also refer to dose conversion for different animals. More
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MSC2530818 1883423-59-3 Cell Cycle/Checkpoint CDK Cyclin dependent kinase MSC-2530818 Inhibitor MSC 2530818 inhibit inhibitor