| Size | Price | Stock | Qty |
|---|---|---|---|
| 5mg |
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| Other Sizes |
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| ln Vitro |
The inability of DCs and macrophages to produce proinflammatory mediators in response to Mycobacterium bovis and Mycobacterium tuberculosis is caused by IRAK-4 deficiency. E stimulated IRAK-4-/- cells. Coli LPS demonstrated a considerable decrease in p65 phosphorylation as well as delayed activation kinetics of all examined signaling proteins [1]. IRAK1/4 (20 μM) inhibits the production of IL-6 mediated by LPS. IRAK1/4 inhibitors do not cause AM to have less p38 phosphorylation. The combination of IRAK1/4 and Rip2 inhibitors inhibits TLR2-mediated cytokine production in sarcoidosis PBMCs and AMs [2]. IRAK4 is overexpressed and activated in T-ALL. When patient T-ALL cells are compared to thymic or peripheral blood T cells, IRAK4 mRNA levels are higher [3].
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| ln Vivo |
In comparison to IRAK-4+/+ or IRAK-4+/-mice, IRAK-4-/- mice exhibited a markedly decreased survival rate following aerosol infection. In all organs at 15, 30, and 60 days after infection, the bacterial burden is higher in IRAK-4-/-mice [1]. Combination therapy using IRAK1/4 inhibitors and ABT-737 has been shown to be more effective in treating MCL1 but not BCL-xL in vivo [3].
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| References |
[1]. Marinho FV, et al. Lack of IL-1 Receptor-Associated Kinase-4 Leads to Defective Th1 Cell Responses and Renders Mice Susceptible to Mycobacterial Infection. J Immunol. 2016 Sep 1;197(5):1852-63.
[2]. Talreja J, et al. Dual Inhibition of Rip2 and IRAK1/4 Regulates IL-1β and IL-6 in Sarcoidosis Alveolar Macrophages and Peripheral Blood Mononuclear Cells. J Immunol. 2016 Aug 15;197(4):1368-78. [3]. Li Z, et al. Inhibition of IRAK1/4 sensitizes T cell acute lymphoblastic leukemia to chemotherapies. J Clin Invest. 2015 Mar 2;125(3):1081-97 |
| Molecular Formula |
C33H35N6O3F3
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|---|---|
| Molecular Weight |
620.6646
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| CAS # |
1012104-68-5
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| Related CAS # |
IRAK inhibitor 4 (trans);2070014-89-8
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| SMILES |
OC1CCC(N2C3=C(C=C(C=C3)C(NCCC(C)C)=O)N=C2NC4=NNC5=C4C=C(C=C5)C6=CC=CC=C6OC(F)(F)F)CC1
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| Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month |
| Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
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| Solubility (In Vitro) |
DMSO : ~12.5 mg/mL (~20.14 mM)
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|---|---|
| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 1.25 mg/mL (2.01 mM) (saturation unknown) in 10% DMSO + 40% PEG300 + 5% Tween80 + 45% Saline (add these co-solvents sequentially from left to right, and one by one), clear solution.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 12.5 mg/mL clear DMSO stock solution to 400 μL PEG300 and mix evenly; then add 50 μL Tween-80 to the above solution and mix evenly; then add 450 μL normal saline to adjust the volume to 1 mL. Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH₂ O to obtain a clear solution. Solubility in Formulation 2: ≥ 1.25 mg/mL (2.01 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one), clear solution. For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 12.5 mg/mL clear DMSO stock solution to 900 μL of corn oil and mix evenly. (Please use freshly prepared in vivo formulations for optimal results.) |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 1.6112 mL | 8.0559 mL | 16.1119 mL | |
| 5 mM | 0.3222 mL | 1.6112 mL | 3.2224 mL | |
| 10 mM | 0.1611 mL | 0.8056 mL | 1.6112 mL |
*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.
Calculation results
Working concentration： mg/mL；
Method for preparing DMSO stock solution： mg drug pre-dissolved in μL DMSO (stock solution 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 stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O，mix and clarify.
(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
(2) Be sure to add the solvent(s) in order.
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