| Size | Price | Stock | Qty |
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| 1mg |
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| 5mg |
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| 10mg |
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| 100mg |
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| 500mg | |||
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| Other Sizes |
| Targets |
WAY-646458 specifically targets casein kinase 1d (CK1δ). It acts as an inhibitor of this serine/threonine kinase, blocking its enzymatic activity and thereby modulating downstream signaling pathways regulated by CK1δ.
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| ln Vitro |
In vitro, WAY-646458 inhibits casein kinase 1δ activity. As a CK1δ inhibitor, it is expected to reduce the phosphorylation of CK1δ substrates, thereby modulating signaling pathways. Specific IC50 values and detailed activity data are limited in publicly available sources.
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| ln Vivo |
In vivo activity of WAY-646458 has been investigated in preclinical models. By inhibiting CK1δ, the compound may modulate downstream signaling pathways and produce therapeutic effects in disease models. Specific in vivo efficacy data is limited, as the compound is primarily used as a research tool.
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| Enzyme Assay |
The inhibitory activity of WAY-646458 against CK1δ is assessed using kinase activity assays. Recombinant human CK1δ enzyme is incubated with a peptide substrate and ATP in the presence of varying concentrations of the compound. Phosphorylation of the substrate is detected using radiolabeled ATP (³³P-ATP) or fluorescence-based detection methods. IC50 values are calculated from dose-response curves.
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| Cell Assay |
Cellular assays for WAY-646458 involve treating cells with the compound and assessing CK1δ-dependent phosphorylation events. Target engagement is confirmed by measuring the phosphorylation levels of known CK1δ substrates by Western blotting using phospho-specific antibodies. Cell viability and proliferation assays are performed to evaluate phenotypic effects.
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| Animal Protocol |
In vivo studies of WAY-646458 are conducted in rodent models of diseases where CK1δ is implicated. The compound is administered via intraperitoneal (i.p.) injection or oral gavage. Endpoints depend on the disease model being studied and may include assessment of pathway modulation, disease severity, and histopathological analysis.
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| ADME/Pharmacokinetics |
Pharmacokinetic properties of WAY-646458 (molecular weight 262.26) are evaluated in rodents following administration. The compound is formulated in suitable vehicles for in vivo administration. Plasma concentrations are measured using LC-MS/MS to determine key PK parameters including oral bioavailability and half-life.
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| Toxicity/Toxicokinetics |
WAY-646458 is intended for research use only and is not approved for clinical use. Standard toxicology assessments would include acute and repeat-dose toxicity studies in rodents. No specific toxicity data is available in the public domain for this compound.
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| Additional Infomation |
WAY-646458 is a research tool for studying the role of casein kinase 1δ in cellular signaling and disease. CK1δ is a multifunctional kinase involved in the regulation of circadian rhythms, Wnt/β-catenin signaling, and other cellular processes. Inhibitors of CK1δ are being investigated as potential therapeutic agents for various diseases.
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| Molecular Formula |
C16H10N2O2
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|---|---|
| Molecular Weight |
262.262803554535
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| Exact Mass |
262.07
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| Elemental Analysis |
C, 73.27; H, 3.84; N, 10.68; O, 12.20
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| CAS # |
852413-92-4
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| PubChem CID |
2564678
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| Appearance |
Typically exists as solid at room temperature
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| LogP |
3.8
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| Hydrogen Bond Donor Count |
0
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| Hydrogen Bond Acceptor Count |
4
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| Rotatable Bond Count |
2
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| Heavy Atom Count |
20
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| Complexity |
332
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| Defined Atom Stereocenter Count |
0
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| SMILES |
C1=CC=C2C(=C1)C3=C(O2)C=CC(=C3)OC4=NC=CC=N4
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| InChi Key |
YCVUYMXARYOMIQ-UHFFFAOYSA-N
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| InChi Code |
InChI=1S/C16H10N2O2/c1-2-5-14-12(4-1)13-10-11(6-7-15(13)20-14)19-16-17-8-3-9-18-16/h1-10H
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| Chemical Name |
2-(Dibenzo[b,d]furan-2-yloxy)pyrimidine
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| Synonyms |
WAY-646458; WAY 646458; WAY646458
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| HS Tariff Code |
2934.99.9001
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| Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month |
| Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
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| Solubility (In Vitro) |
May dissolve in DMSO (in most cases), if not, try other solvents such as H2O, Ethanol, or DMF with a minute amount of products to avoid loss of samples
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| Solubility (In Vivo) |
Note: Listed below are some common formulations that may be used to formulate products with low water solubility (e.g. < 1 mg/mL), you may test these formulations using a minute amount of products to avoid loss of samples.
Injection Formulations
Injection Formulation 1: DMSO : Tween 80： Saline = 10 : 5 : 85 (i.e. 100 μL DMSO stock solution → 50 μL Tween 80 → 850 μL Saline)(e.g. IP/IV/IM/SC) *Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH ₂ O to obtain a clear solution. Injection Formulation 2: DMSO : PEG300 ：Tween 80 : Saline = 10 : 40 : 5 : 45 (i.e. 100 μL DMSO → 400 μLPEG300 → 50 μL Tween 80 → 450 μL Saline) Injection Formulation 3: DMSO : Corn oil = 10 : 90 (i.e. 100 μL DMSO → 900 μL Corn oil) Example: Take the Injection Formulation 3 (DMSO : Corn oil = 10 : 90) as an example, if 1 mL of 2.5 mg/mL working solution is to be prepared, you can take 100 μL 25 mg/mL DMSO stock solution and add to 900 μL corn oil, mix well to obtain a clear or suspension solution (2.5 mg/mL, ready for use in animals). View More
Injection Formulation 4: DMSO : 20% SBE-β-CD in saline = 10 : 90 [i.e. 100 μL DMSO → 900 μL (20% SBE-β-CD in saline)] Oral Formulations
Oral Formulation 1: Suspend in 0.5% CMC Na (carboxymethylcellulose sodium) Oral Formulation 2: Suspend in 0.5% Carboxymethyl cellulose Example: Take the Oral Formulation 1 (Suspend in 0.5% CMC Na) as an example, if 100 mL of 2.5 mg/mL working solution is to be prepared, you can first prepare 0.5% CMC Na solution by measuring 0.5 g CMC Na and dissolve it in 100 mL ddH2O to obtain a clear solution; then add 250 mg of the product to 100 mL 0.5% CMC Na solution, to make the suspension solution (2.5 mg/mL, ready for use in animals). View More
Oral Formulation 3: Dissolved in PEG400 (Please use freshly prepared in vivo formulations for optimal results.) |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 3.8130 mL | 19.0650 mL | 38.1301 mL | |
| 5 mM | 0.7626 mL | 3.8130 mL | 7.6260 mL | |
| 10 mM | 0.3813 mL | 1.9065 mL | 3.8130 mL |
*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.
Calculation results
Working concentration： mg/mL；
Method for preparing DMSO stock solution： mg drug pre-dissolved in μL DMSO (stock solution concentration mg/mL). Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug.
Method for preparing in vivo formulation:：Take μL DMSO stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O，mix and clarify.
(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.
(2) Be sure to add the solvent(s) in order.
Products are for research use only; We do not sell to patients
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