Londamocitinib
Based on 1 Customer Validation
Londamocitinib (AZD4604) is a potent and selective JAK1 inhibitor with IC50 at 0.54 nM. Londamocitinib has anti-inflammatory activity.
For research use only. We do not sell to patients.
- Purity: 99.79%
- CAS No.: 2241039-81-4
- Formula: C28H31F2N7O4S
- Molecular Weight:599.65
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Storage:Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 6 months , -20°C, 1 month
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Biological Activity
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Chemical Information
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Solvent & Solubility
- Purity & Documentation
- References
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Help & FAQs
Biological Activity
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JAK1 0.54 nM (IC50) |
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:OVA-Induced Rat Model of Asthma[3]
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Dosage:1 mg/kg
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Administration:i.v.
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Result:Reduced the proportion of phosphorylated STAT3-positive cell nuclei.
| NCT Number | Sponsor | Condition | Start Date |
Phase
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|---|---|---|---|---|
| NCT01329991 | Plexxikon| | 2011-05 | PHASE1 |
Chemical Information
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CAS No. 2241039-81-4
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Appearance Solid
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Molecular Weight 599.65
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Formula C28H31F2N7O4S
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Color White to off-white
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SMILES
FC1=C(S(C)(=O)=O)C=CC=C1NC2=NC(C3=CNC4=C3C=CC=C4NC([C@@H](COC)N5CCN(C)CC5)=O)=C(F)C=N2
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Synonyms
AZD4604; JAK1-IN-7
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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 6 months -20°C 1 month
Solvent & Solubility
DMSO : 71.43 mg/mL (119.12 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. 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. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
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: ≥ 2.5 mg/mL (4.17 mM); Clear solution
This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 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.
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 (272 KB)
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SDS (419 KB)
- English - EN (419 KB)
- Français - FR (419 KB)
- Deutsch - DE (419 KB)
- Norwegian - NO (419 KB)
- Español - ES (419 KB)
- Swedish - SV (419 KB)
- Italian - IT (419 KB)
- Portuguese - PT (419 KB)
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Handling Instructions (2659 KB)
References
[1]. NILSSON, Karl, Magnus, et al. Jak1 selective inhibitors. WO2018134213A1.
[2]. Nilsson M, et al. Discovery of the Potent and Selective Inhaled Janus Kinase 1 Inhibitor AZD4604 and Its Preclinical Characterization. J Med Chem. 2023 Oct 12;66(19):13400-13415. [Content Brief]
[3]. Nilsson M, et al. Characterization of Selective and Potent JAK1 Inhibitors Intended for the Inhaled Treatment of Asthma. Drug Des Devel Ther. 2022 Aug 31;16:2901-2917. [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. 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 | 1.6676 mL | 8.3382 mL | 16.6764 mL | 41.6910 mL |
| 5 mM | 0.3335 mL | 1.6676 mL | 3.3353 mL | 8.3382 mL | |
| 10 mM | 0.1668 mL | 0.8338 mL | 1.6676 mL | 4.1691 mL | |
| 15 mM | 0.1112 mL | 0.5559 mL | 1.1118 mL | 2.7794 mL | |
| 20 mM | 0.0834 mL | 0.4169 mL | 0.8338 mL | 2.0845 mL | |
| 25 mM | 0.0667 mL | 0.3335 mL | 0.6671 mL | 1.6676 mL | |
| 30 mM | 0.0556 mL | 0.2779 mL | 0.5559 mL | 1.3897 mL | |
| 40 mM | 0.0417 mL | 0.2085 mL | 0.4169 mL | 1.0423 mL | |
| 50 mM | 0.0334 mL | 0.1668 mL | 0.3335 mL | 0.8338 mL | |
| 60 mM | 0.0278 mL | 0.1390 mL | 0.2779 mL | 0.6948 mL | |
| 80 mM | 0.0208 mL | 0.1042 mL | 0.2085 mL | 0.5211 mL | |
| 100 mM | 0.0167 mL | 0.0834 mL | 0.1668 mL | 0.4169 mL |
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