IRAK inhibitor 1 (Synonyms: IRAK4-IN-1) |
Catalog No.GC17158 |
An IRAK4 inhibitor
Products are for research use only. Not for human use. We do not sell to patients.
Cas No.: 1042224-63-4
Sample solution is provided at 25 µL, 10mM.
Quality Control & SDS
- View current batch:
- Purity: >99.00%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
- Datasheet
IC50: 35 nM for IRAK-4
The interleukin-1 receptor associated kinase (IRAK) family is comprised of four family members IRAK-1, IRAK-2, IRAK-3/M, and IRAK-4. Upon activation of their upstream cognate receptors, IRAK-4 is thought to phosphorylate IRAK-1 resulting in the activation and autophosphorylation of IRAK-1 an subsequent phosphorylation of downstream substrates. IRAK inhibitor 1 is an inhibitor of interleukin-1 receptor associated kinase 4 (IRAK-4).
In vitro: The regioisomeric pyridines IRAK inhibitor 1 (6) and it analogue (7) showed contrasting SAR, with the 2,6-pyridine isomer IRAK inhibitor 1 having low-nanomolar potency whilst the 2,4-pyridine isomer 7 showed little activity, despite having a more accessible bidentate-binding motif. At 10 μM, IRAK inhibitor 1 was found to have 39% inhibition for JNK-1 and 15% inhibition for JNK-2, respectivley [1].
In vivo: No animal in-vivo data available currently IRAK inhibitor 1 and its analogues.
Clinical trial: IRAK inhibitor 1 is currently in the preclinical development stage and no clinical data are available.
Reference:
[1] Buckley GM, Ceska TA, Fraser JL, Gowers L, Groom CR, Higueruelo AP, Jenkins K, Mack SR, Morgan T, Parry DM, Pitt WR, Rausch O, Richard MD, Sabin V. IRAK-4 inhibitors. Part II: a structure-based assessment of imidazo[1,2-a]pyridine binding. Bioorg Med Chem Lett. 2008;18(11):3291-5.
Cas No. | 1042224-63-4 | SDF | |
Synonyms | IRAK4-IN-1 | ||
Chemical Name | 6-imidazo[1,2-a]pyridin-3-yl-N-piperidin-4-ylpyridin-2-amine | ||
Canonical SMILES | C1CNCCC1NC2=CC=CC(=N2)C3=CN=C4N3C=CC=C4 | ||
Formula | C17H19N5 | M.Wt | 293.37 |
Solubility | Soluble in DMSO | Storage | Store at -20°C |
General tips | Please select the appropriate solvent to prepare the stock solution according to the
solubility of the product in different solvents; once the solution is prepared, please store it in
separate packages to avoid product failure caused by repeated freezing and thawing.Storage method
and period of the stock solution: When stored at -80°C, please use it within 6 months; when stored
at -20°C, please use it within 1 month. To increase solubility, heat the tube to 37°C and then oscillate in an ultrasonic bath for some time. |
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Shipping Condition | Evaluation sample solution: shipped with blue ice. All other sizes available: with RT, or with Blue Ice upon request. |
Prepare stock solution | |||
1 mg | 5 mg | 10 mg | |
1 mM | 3.4087 mL | 17.0433 mL | 34.0866 mL |
5 mM | 0.6817 mL | 3.4087 mL | 6.8173 mL |
10 mM | 0.3409 mL | 1.7043 mL | 3.4087 mL |
Step 1: Enter information below (Recommended: An additional animal making an allowance for loss during the experiment)
Step 2: Enter the in vivo formulation (This is only the calculator, not formulation. Please contact us first if there is no in vivo formulation at the solubility Section.)
Calculation results:
Working concentration: mg/ml;
Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid 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 master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O, mix and clarify.
Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.
Note: 1. Please make sure the liquid is clear before adding the next solvent.
2. Be sure to add the solvent(s) in order. You must ensure that the solution obtained, in the previous addition, is a clear solution before proceeding to add the next solvent. Physical methods such as vortex, ultrasound or hot water bath can be used to aid dissolving.
3. All of the above co-solvents are available for purchase on the GlpBio website.
Average Rating: 5
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