| Size | Price | Stock | Qty |
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| 1mg |
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| 5mg |
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| 10mg |
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| Targets |
DK419 targets the Wnt/β-catenin signaling pathway. It reduces protein levels of Axin2, β-catenin, c-Myc, Cyclin D1 and Survivin. It also induces production of pAMPK. It alters cellular oxygen consumption rate.
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|---|---|
| ln Vitro |
In vitro, DK419 inhibits Wnt/β-catenin signaling with an IC50 of 0.19 μM. It reduces protein levels of Axin2, β-catenin, c-Myc, Cyclin D1 and Survivin. It induces production of pAMPK.
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| ln Vivo |
In vivo, DK419 is an orally active inhibitor of Wnt/β-catenin signaling. It has anticancer activity and inhibits colorectal cancer growth.
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| Enzyme Assay |
In vitro assays for DK419 typically measure its ability to inhibit Wnt/β-catenin signaling. Reporter gene assays using cells transfected with a Wnt-responsive luciferase reporter are used. Protein levels of downstream targets are measured by Western blot.
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| Cell Assay |
Cell-based assays for DK419 involve treating cancer cells with the compound and measuring cell proliferation, apoptosis, and Wnt/β-catenin signaling. The compound's effects on protein levels and signaling pathways are assessed.
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| Animal Protocol |
In vivo animal studies for DK419 typically involve oral administration to mouse models of colorectal cancer. Tumor growth is monitored, and the compound's ability to inhibit tumor growth is assessed.
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| ADME/Pharmacokinetics |
Pharmacokinetic properties of DK419 are characteristic of orally active small molecules. The compound is absorbed following oral administration. Its half-life and tissue distribution have been studied in preclinical models.
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| Toxicity/Toxicokinetics |
The toxicological profile of DK419 has not been extensively characterized. As a research compound, it should be handled with appropriate safety precautions.
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| References | |
| Additional Infomation |
DK419 is a research tool for studying the Wnt/β-catenin signaling pathway and its role in cancer. It is not approved for therapeutic use. The compound is valuable for investigating the potential of targeting Wnt/β-catenin signaling for cancer therapy.
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| Molecular Formula |
C16H8CLF6N3O
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|---|---|
| Molecular Weight |
407.6976
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| Exact Mass |
407.026
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| CAS # |
2102672-22-8
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| PubChem CID |
44536362
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| Appearance |
White to off-white solid powder
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| LogP |
4.8
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| Hydrogen Bond Donor Count |
2
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| Hydrogen Bond Acceptor Count |
8
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| Rotatable Bond Count |
2
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| Heavy Atom Count |
27
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| Complexity |
549
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| Defined Atom Stereocenter Count |
0
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| SMILES |
ClC1=C([H])C(C(N([H])C2C([H])=C([H])C(C(F)(F)F)=C([H])C=2[H])=O)=C2C(=C1[H])N([H])C(C(F)(F)F)=N2
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| InChi Key |
MWNNIGRGNSXNEA-UHFFFAOYSA-N
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| InChi Code |
InChI=1S/C16H8ClF6N3O/c17-8-5-10(12-11(6-8)25-14(26-12)16(21,22)23)13(27)24-9-3-1-7(2-4-9)15(18,19)20/h1-6H,(H,24,27)(H,25,26)
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| Chemical Name |
6-chloro-2-(trifluoromethyl)-N-[4-(trifluoromethyl)phenyl]-1H-benzimidazole-4-carboxamide
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| Synonyms |
DK 419 DK-419 DK419
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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) |
DMSO : ~83.33 mg/mL (~204.39 mM)
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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 | 2.4528 mL | 12.2639 mL | 24.5278 mL | |
| 5 mM | 0.4906 mL | 2.4528 mL | 4.9056 mL | |
| 10 mM | 0.2453 mL | 1.2264 mL | 2.4528 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.
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