Longdaysin
Based on 1 Customer Validation
Longdaysin is a inhibitor of the Wnt/β-catenin signaling pathway, which exerts antitumor effect through blocking CK1δ/ε-dependent Wnt signaling. Longdaysin inhibits CK1α, CK1δ, CDK7, and ERK2 with IC50s of 5.6 µM, 8.8 µM, 29 µM, and 52 µM, respectively.
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- Reinheit: 99.83%
- CAS. Nr.: 1353867-91-0
- Formel: C16H16F3N5
- Molecular Weight:335.33
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Speicherung:
4°C, protect from light
* In solvent : -80°C, 6 months; -20°C, 1 month (protect from light)
To place orders, for customer services and technical support, please contact: MedChemExpress USA
Tel: 609-228-6898 E-mail: [email protected] [email protected]
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Biologische Aktivität
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Chemical Information
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Lösungsmittel & Löslichkeit
- Reinheit & Dokumentation
- Verweise
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Help & FAQs
Biologische Aktivität
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CK1α/CSNK1A1 5.6 μM (IC50) |
CK1δ 8.8 μM (IC50) |
CDK7 29 μM (IC50) |
ERK2 52 μM (IC50) |
Longdaysin (0-9 µM; 1 week) lengthens circadian period in adult tail fibroblasts, lung explants, and SCN explants from mPer2Luc knockin mice[2].
Longdaysin (0-25 µM; 1 week ) inhibits the colony formation, migration, invasion, and sphere formation of breast cancer Hs578T or MDA-MB-231 cells[3].
Longdaysin (0-50 µM; 24 h) inhibits Wnt/β-catenin signaling by inhibition of CK1δ and CK1ε in HEK293T cells[3].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:HEK293T cells
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Concentration:0-50 µM
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Incubation Time:24 h
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Result:Reduced the levels of phosphorylated LRP6, total LRP6, phosphorylated DVL2, activated β-catenin, and total β-catenin.
Longdaysin (5 mg/kg, i.p., every 3 days for 3 weeks) inhibits tumor growth in MDA-MB-231 xenografts mice[3].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:MDA-MB-231 xenografts[3]
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Dosage:5 mg/kg
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Administration:i.p., every 3 days for 3 weeks
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Result:Decreased tumor cell density and proliferation (indicated by Ki-67).
Reduced the expression of active and total β-catenin, and decreased the expression of phosphorylated and total LRP6, phosphorylated DVL2, and active and total β-catenin.
Reduced mRNA expression of the Wnt target genes including Axin2, DKK1, LEF1, and Survivin.
Chemical Information
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CAS. Nr. 1353867-91-0
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Appearance Solid
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Molecular Weight 335.33
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Formel C16H16F3N5
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Color White to off-white
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SMILES
FC(F)(F)C1=CC=CC(CNC2=NC=NC3=C2N=CN3C(C)C)=C1
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Versand
Room temperature in continental US; may vary elsewhere.
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Speicherung
4°C, protect from light
* In solvent : -80°C, 6 months; -20°C, 1 month (protect from light)
Lösungsmittel & Löslichkeit
DMSO : 125 mg/mL (372.77 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (protect from light). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (protect from light). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
Konzentration (Stammlösung) × Volumen (Stammlösung) = Konzentration (Ziellösung) × Volumen (Ziellösung)
Select the appropriate dissolution method based on your experimental animal and administration route.
- For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
- To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for In Vivo experiments, it is recommended to prepare freshly and use it on the same day.
- The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.
Add each solvent one by one: 10% DMSO 40% PEG300 5% Tween-80 45% Saline
Solubility: ≥ 2.08 mg/mL (6.20 mM); Clear solution
This protocol yields a clear solution of ≥ 2.08 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (20.8 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.
Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
Please enter the basic information of animal experiments:
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Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
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%DMSO +
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
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%+
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+%Tween-80 + +
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%Saline +
The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).
Working solution concentration: 0.22 mg/mL
Method for preparing stock solution: mg drug dissolved in μL DMSO. Stock solution concentration: mg/mL. * In solvent : -80°C, 6 months; -20°C, 1 month (protect from light)
1. Take μL DMSO stock solution;
2. Add μL .
μL , mix evenly;
3. Then add μL Tween 80, mix evenly;
4. Then add μL
Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.
Reinheit & Dokumentation
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Data Sheet (276 KB)
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SDS (393 KB)
- English - EN (393 KB)
- Français - FR (393 KB)
- Deutsch - DE (393 KB)
- Norwegian - NO (393 KB)
- Español - ES (393 KB)
- Swedish - SV (393 KB)
- Italian - IT (393 KB)
- Korean - KR (393 KB)
- Portuguese - PT (393 KB)
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Handling Instructions (2659 KB)
Verweise
[2]. Hirota T, et al. High-throughput chemical screen identifies a novel potent modulator of cellular circadian rhythms and reveals CKIα as a clock regulatory kinase. PLoS Biol. 2010 Dec 14;8(12):e1000559. [Content Brief]
[3]. Xiong Y, et al. Longdaysin inhibits Wnt/β-catenin signaling and exhibits antitumor activity against breast cancer. Onco Targets Ther. 2019 Feb 5;12:993-1005. [Content Brief]
Complete Stock Solution Preparation Table
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (protect from light). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
| Optional Solvent | Concentration Solvent Mass | 1 mg | 5 mg | 10 mg | 25 mg |
|---|---|---|---|---|---|
| DMSO | 1 mM | 2.9821 mL | 14.9107 mL | 29.8214 mL | 74.5534 mL |
| 5 mM | 0.5964 mL | 2.9821 mL | 5.9643 mL | 14.9107 mL | |
| 10 mM | 0.2982 mL | 1.4911 mL | 2.9821 mL | 7.4553 mL | |
| 15 mM | 0.1988 mL | 0.9940 mL | 1.9881 mL | 4.9702 mL | |
| 20 mM | 0.1491 mL | 0.7455 mL | 1.4911 mL | 3.7277 mL | |
| 25 mM | 0.1193 mL | 0.5964 mL | 1.1929 mL | 2.9821 mL | |
| 30 mM | 0.0994 mL | 0.4970 mL | 0.9940 mL | 2.4851 mL | |
| 40 mM | 0.0746 mL | 0.3728 mL | 0.7455 mL | 1.8638 mL | |
| 50 mM | 0.0596 mL | 0.2982 mL | 0.5964 mL | 1.4911 mL | |
| 60 mM | 0.0497 mL | 0.2485 mL | 0.4970 mL | 1.2426 mL | |
| 80 mM | 0.0373 mL | 0.1864 mL | 0.3728 mL | 0.9319 mL | |
| 100 mM | 0.0298 mL | 0.1491 mL | 0.2982 mL | 0.7455 mL |
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