MSC2530818
This product is for research use only, not for human use. We do not sell to patients.
For small sizes, please check our retail website as below: www.invivochem.com
| Size | Price | Stock |
|---|---|---|
| 250mg | $1880 | Check With Us |
| 500mg | $2500 | Check With Us |
| 1g | $3750 | Check With Us |
: Cat #: V2742 CAS #: 1883423-59-3 Purity ≥ 98%
Description: MSC2530818 is novel, potent, selective and orally available small molecule inhibitor of cyclin dependent kinase CDK8 with the IC50 of 2.6 nM.
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| Molecular Weight (MW) | 340.81 |
|---|---|
| Molecular Formula | C18H17ClN4O |
| CAS No. | 1883423-59-3 |
| Storage | -20℃ for 3 years in powder formr |
| -80℃ for 2 years in solvent | |
| Solubility In Vitro | DMSO: > 70 mg/mLr |
| Water: <1 mg/mLr | |
| Ethanol: > 70 mg/mL | |
| SMILES Code | O=C(N1[C@H](C2=CC=C(Cl)C=C2)CCC1)C3=CN=C(NN=C4C)C4=C3 |
| Synonyms | MSC-2530818; MSC2530818; MSC 2530818 |
| Protocol | In Vitro | MSC2530818 binds to CDK8 and CDK19 with 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). 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 |
These protocols are for reference only. InvivoChem does not
independently validate these methods.
| Solvent volume to be added | Mass (the weight of a compound) | |||
|---|---|---|---|---|
| Mother liquor concentration | 1mg | 5mg | 10mg | 20mg |
| 1mM | 2.9342 mL | 14.6709 mL | 29.3419 mL | 58.6837 mL |
| 5mM | 0.5868 mL | 2.9342 mL | 5.8684 mL | 11.7367 mL |
| 10mM | 0.2934 mL | 1.4671 mL | 2.9342 mL | 5.8684 mL |
| 20mM | 0.1467 mL | 0.7335 mL | 1.4671 mL | 2.9342 mL |
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Step Two: Enter the in vivo formulation
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Method for preparing DMSO master liquid:
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,Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug.
Method for preparing in vivo formulation:
Take
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DMSO master liquid, next add
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PEG300, mix and clarify, next add
µL
Tween 80,mix and clarify, next add
µL
ddH2O,mix and clarify.
Note:
- (1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
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