CE-245677
Based on 1 Customer Validation
CE-245677 is a selective, reversible TrkA/B and Tie2 inhibitor. CE-245677 is effective in multiple pain models and inhibits tumor growth and the proliferation of Plasmodium falciparum during the erythrocytic stage.
For research use only. We do not sell to patients.
- Purity : 98.00%
- CAS No.: 717899-97-3
- Formula: C24H22Cl2N6O3
- Molecular Weight:513.38
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Storage:Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 2 years , -20°C, 1 year
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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Biological Activity
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Chemical Information
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Solvent & Solubility
- Protocols
- Purity & Documentation
- References
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Help & FAQs
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Biological Activity
Description
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TrkA |
TrkB |
Tie2 |
Plasmodium |
In Vitro
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Chemical Information
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CAS No. 717899-97-3
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Appearance Solid
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Molecular Weight 513.38
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Formula C24H22Cl2N6O3
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Color White to off-white
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SMILES
O=C(NC1=CC=C(Cl)C=C1Cl)NC2=CC(C(C3=CN(C(C)C)C4=NC=NC(N)=C43)=O)=CC=C2OC
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Shipping
Room temperature in continental US; may vary elsewhere.
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Storage
Powder -20°C 3 years 4°C 2 years In solvent -80°C 2 years -20°C 1 year
Solvent & Solubility
In Vitro:
DMSO : 125 mg/mL (243.48 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, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.
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, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
In Vivo:
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 (4.05 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.
In Vivo Dissolution Calculator
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.
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.
Purity & Documentation
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Data Sheet (285 KB)
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SDS (396 KB)
- English - EN (396 KB)
- Français - FR (396 KB)
- Deutsch - DE (396 KB)
- Norwegian - NO (396 KB)
- Español - ES (396 KB)
- Swedish - SV (396 KB)
- Italian - IT (396 KB)
- Korean - KR (396 KB)
- Portuguese - PT (396 KB)
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Handling Instructions (2659 KB)
References
[1]. Bagal SK, et al. Discovery of Potent, Selective, and Peripherally Restricted Pan-Trk Kinase Inhibitors for the Treatment of Pain. Journal of medicinal chemistry. 2018 Aug 09;61(15):6779-6800. [Content Brief]
[2]. Yamada T, et al. Discovery and hit to lead optimization of macrocyclic peptides as novel tropomyosin receptor kinase A antagonists. Journal of Medicinal Chemistry. 2024 Jul 1;67(13):11197-208. [Content Brief]
[7]. Skerratt SE, et al. The Discovery of a Potent, Selective, and Peripherally Restricted Pan-Trk Inhibitor (PF-06273340) for the Treatment of Pain. Journal of medicinal chemistry. 2016 Nov 23;59(22):10084-10099. [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, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.
| Optional Solvent | Concentration Solvent Mass | 1 mg | 5 mg | 10 mg | 25 mg |
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| DMSO | 1 mM | 1.9479 mL | 9.7394 mL | 19.4787 mL | 48.6969 mL |
| 5 mM | 0.3896 mL | 1.9479 mL | 3.8957 mL | 9.7394 mL | |
| 10 mM | 0.1948 mL | 0.9739 mL | 1.9479 mL | 4.8697 mL | |
| 15 mM | 0.1299 mL | 0.6493 mL | 1.2986 mL | 3.2465 mL | |
| 20 mM | 0.0974 mL | 0.4870 mL | 0.9739 mL | 2.4348 mL | |
| 25 mM | 0.0779 mL | 0.3896 mL | 0.7791 mL | 1.9479 mL | |
| 30 mM | 0.0649 mL | 0.3246 mL | 0.6493 mL | 1.6232 mL | |
| 40 mM | 0.0487 mL | 0.2435 mL | 0.4870 mL | 1.2174 mL | |
| 50 mM | 0.0390 mL | 0.1948 mL | 0.3896 mL | 0.9739 mL | |
| 60 mM | 0.0325 mL | 0.1623 mL | 0.3246 mL | 0.8116 mL | |
| 80 mM | 0.0243 mL | 0.1217 mL | 0.2435 mL | 0.6087 mL | |
| 100 mM | 0.0195 mL | 0.0974 mL | 0.1948 mL | 0.4870 mL |
CE-245677 Related Classifications
HY-112423 Related Classifications
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