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MSC2530818

產(chǎn)品活性：MSC2530818是有效，選擇性，有口服活性的 CDK8 抑制劑，抑制 CDK8 的IC₅₀值為2.6 nM。

研究領(lǐng)域：Cell Cycle/DNA Damage

作用靶點(diǎn)：CDK

In Vitro: MSC2530818 binds to CDK8 and CDK19 with similar affinity (4 nM). Potent inhibition of phospho-STAT1^SER727, an established biomarker of CDK8 activity, in SW620 human colorectal carcinoma cells is also observed (pSTAT1^SER727 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). MSC2530818 demonstrates minimal activity in the CEREP panel, and demonstrates minimal hERG inhibition. Furthermore, MSC2530818 is a soluble CDK8 inhibitor with high permeability and low efflux ratio in Caco-2 cells and does not inhibit any cytochrome P450 subtypes.

In Vivo: Tumor-bearing mice treated with MSC2530818 shows 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 may be ≥75% up to dose level of 500 mg daily.

相關(guān)產(chǎn)品：Bioactive Compound Library Plus  |  Cell Cycle/DNA Damage Compound Library  |  Kinase Inhibitor Library  |  Anti-Cancer Compound Library  |  Anti-Aging Compound Library  |  Orally Active Compound Library  |  Anti-Breast Cancer Compound Library  |  Anti-Blood Cancer Compound Library  |  Targeted Diversity Library  |  Cancer Stem Cells Compound Library  |  Heterocyclic Compound Library  |  Membrane Protein-targeted Compound Library  |  SY-5609  |  CLK1/2-IN-1  |  SB-218078  |  Toyocamycin  |  (S)-LY3177833 hydrate  |  Dinaciclib  |  EGFR/HER2/CDK9-IN-2  |  CDK8-IN-11  |  SNS-032  |  M2N12  |  Palbociclib-d₈  |  EGFR/CDK2-IN-1  |  BSJ-04-132  |  (E/Z)-Zotiraciclib  |  CCT-251921  |  BS-181  |  Ribociclib-d₈  |  CDK9-IN-9  |  Flavopiridol  |  SRI-29329  |  dCeMM4  |  GSK 3 Inhibitor IX  |  CDK9-IN-7  |  BSJ-03-204  |  Amantadine-d₆  |  K00546  |  Abemaciclib metabolite M18 hydrochloride  |  Ribociclib-d₆  |  Lacto-N-fucopentaose I  |  CDK2/4/6-IN-2

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