Lck inhibitor 2
Based on 1 Customer Validation
Lck inhibitor 2 is a multi-target tyrosine kinase inhibitor with IC50s of 13nM, 9nM, 3nM, 26nM and 2nM for Lck, Btk, Lyn, Btk and Txk respectively.
For research use only. We do not sell to patients.
- Purity: 99.73%
- CAS No.: 944795-06-6
- Formula: C18H17N5O2
- Molecular Weight:335.36
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Storage:Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 2 years , -20°C, 1 year
Biological Activity
Chemical Information
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CAS No. 944795-06-6
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Appearance Solid
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Molecular Weight 335.36
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Formula C18H17N5O2
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Color Light yellow to yellow
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SMILES
OC1=CC=C(C)C(NC2=CC=NC(NC3=CC(C(N)=O)=CC=C3)=N2)=C1
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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
DMSO : 100 mg/mL (298.19 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)
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 mg/mL (5.96 mM); Clear solution
This protocol yields a clear solution of ≥ 2 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (20.0 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.
Add each solvent one by one: 10% DMSO 90% (20% SBE-β-CD in Saline)
Solubility: ≥ 2 mg/mL (5.96 mM); Clear solution
This protocol yields a clear solution of ≥ 2 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (20.0 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.
Preparation of 20% SBE-β-CD in Saline (4°C, storage for one week): 2 g SBE-β-CD powder is dissolved in 10 mL Saline, completely dissolve until clear.
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 (273 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)
- Portuguese - PT (393 KB)
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Handling Instructions (2659 KB)
References
[1]. Bamborough, et al. Assessment of Chemical Coverage of Kinome Space and Its Implications for Kinase Drug Discovery. Journal of Medicinal Chemistry (2008), 51(24), 7898-7914. [Content Brief]
[2]. Bamborough, Paul, et al. N-4-Pyrimidinyl-1H-indazol-4-amine inhibitors of Lck: Indazoles as phenol isosteres with improved pharmacokinetics. Bioorganic & Medicinal Chemistry Letters (2007), 17(15), 4363-4368. [Content Brief]
[3]. Awale, Mahendra, et al. Molecular docking guided 3D-QSAR CoMFA analysis of N-4-Pyrimidinyl-1H-indazol-4-amine inhibitors of leukocyte-specific protein tyrosine kinase. Journal of Molecular Modeling (2008), 14(10), 937-947. [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 |
|---|---|---|---|---|---|
| DMSO | 1 mM | 2.9819 mL | 14.9094 mL | 29.8187 mL | 74.5468 mL |
| 5 mM | 0.5964 mL | 2.9819 mL | 5.9637 mL | 14.9094 mL | |
| 10 mM | 0.2982 mL | 1.4909 mL | 2.9819 mL | 7.4547 mL | |
| 15 mM | 0.1988 mL | 0.9940 mL | 1.9879 mL | 4.9698 mL | |
| 20 mM | 0.1491 mL | 0.7455 mL | 1.4909 mL | 3.7273 mL | |
| 25 mM | 0.1193 mL | 0.5964 mL | 1.1927 mL | 2.9819 mL | |
| 30 mM | 0.0994 mL | 0.4970 mL | 0.9940 mL | 2.4849 mL | |
| 40 mM | 0.0745 mL | 0.3727 mL | 0.7455 mL | 1.8637 mL | |
| 50 mM | 0.0596 mL | 0.2982 mL | 0.5964 mL | 1.4909 mL | |
| 60 mM | 0.0497 mL | 0.2485 mL | 0.4970 mL | 1.2424 mL | |
| 80 mM | 0.0373 mL | 0.1864 mL | 0.3727 mL | 0.9318 mL | |
| 100 mM | 0.0298 mL | 0.1491 mL | 0.2982 mL | 0.7455 mL |