| Size | Price | Stock | Qty |
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| 1mg |
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| 5mg |
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| 10mg |
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| Other Sizes |
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| ln Vitro |
AZ1495 (compound 28) (10 μM, 1 h) is kinase selective for IRAK4 with IC50 values of 0.005 μM (enzyme assay) and 0.052 μM (cell assay) [1]. AZ1495 (10 μM, 1 h) exhibits a kinase inhibitory effect on IRAK4, with an IC50 value of 0.005 μM and a Kd value of 0.0007 μM[1]. AZ1495 (0.001-100 μM, 72 h) suppresses NF-κB activation and proliferation of ABC-DLBCL cell line in a dose-dependent manner [1]. AZ1495 (0-3.3 μM, 14 hours) coupled with BTK inhibitors in OCI-LY10 cells totally suppresses NF-κB activation and promotes cell death at lower dosages [1].
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| ln Vivo |
AZ1495 (Compound 28) (orally, daily, 12.5 mg/kg) coupled with ibrutinib induced tumor regression in an ABC-DLBCL animal model (OCI-LY10 cells) [1]. AZ1495 (IV, 2 mg/kg and PO, 5 mg/kg) is characterized by high clearance (Cl) in rats (75 mL/min/kg) and moderate prediction based on hepatocyte data (Clint 15 μl /min/106 cells), anticipated clearance rate 42 mL/min/kg), poor bioavailability, consistent with significant first-pass impact [1]. Active renal secretion of AZ1495 (iv, 1 mg/kg) in dogs is low [1].
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| Cell Assay |
Cell Viability Assay[1]
Cell Types: OCI-LY10 and SUDHL2 Cell Tested Concentrations: 0.001-100 μM Incubation Duration: 72 hrs (hours) Experimental Results: Inhibited the growth of OCI-LY10 cells in a dose-dependent manner, while GCB cell line SUDHL2 did not IRAK4 inhibitors are sensitive and do not increase cell killing. Cell death of OCI-LY10 cells increased upon increasing the concentrations of compound 28 and BTK ibrutinib. Western Blot Analysis[1] Cell Types: OCI-LY10 Cell Tested Concentrations: 0-3.3 μM Incubation Duration: 14 h Experimental Results: Inhibited IκBα phosphorylation in a dose-dependent manner in OCI-LY10 cells. Shown that combination with 10 nM ibrutinib induces apoptosis by cleaving caspase 3 in OCI-LY10 cells. |
| Animal Protocol |
Animal/Disease Models: CB.17 SCID (severe combined immunodeficient) mouse [1]
Doses: 12.5 mg/kg Route of Administration: po (po (oral gavage)) daily, 12.5 mg/kg Experimental Results: Single agents have modest antitumor activity, but ibrutinib combination can cause Tumor regression occurred and was well tolerated. Animal/Disease Models: Rat[1] Doses: 2 mg/kg, 5mg/kg Route of Administration: intravenous (iv) (iv)injection, 2 mg/kg and po (po (oral gavage)) 5mg/kg Experimental Results: Species dose (mg/kg) Cl (mL/min/ kg) Vss (L/kg) PO Half-life (h) IV Half-life (h) Fabs (%) F (%) Rat 2,5 75 2.1 2.0 0.8 100 28 Dog 1 29 3.0 - 3.3 - - Animal/Disease Models: dog [1 ] Doses: 1 mg/kg Route of Administration: iv., 1 mg/kg Experimental Results: Type dose (mg/kg) Cl (mL/min/kg) Vss (L/kg) PO half-life (h) IV half-life (h) Fab (%) F (%) Rat 2,5 75 2.1 2.0 0.8 100 28 Dog 1 29 3.0 - 3.3 - - |
| References |
| Molecular Formula |
C21H31N5O2
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|---|---|
| Molecular Weight |
385.50314450264
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| Exact Mass |
385.247
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| CAS # |
2196204-23-4
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| PubChem CID |
131839619
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| Appearance |
White to off-white solid powder
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| LogP |
2.4
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| Hydrogen Bond Donor Count |
2
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| Hydrogen Bond Acceptor Count |
6
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| Rotatable Bond Count |
4
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| Heavy Atom Count |
28
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| Complexity |
489
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| Defined Atom Stereocenter Count |
0
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| SMILES |
O1CCN(CC1)C1CCC(CC1)NC1=C2C(=NC=N1)NC=C2C1CCOCC1
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| InChi Key |
DJVYXMINSBMUHH-UHFFFAOYSA-N
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| InChi Code |
InChI=1S/C21H31N5O2/c1-3-17(26-7-11-28-12-8-26)4-2-16(1)25-21-19-18(15-5-9-27-10-6-15)13-22-20(19)23-14-24-21/h13-17H,1-12H2,(H2,22,23,24,25)
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| Chemical Name |
N-(4-morpholin-4-ylcyclohexyl)-5-(oxan-4-yl)-7H-pyrrolo[2,3-d]pyrimidin-4-amine
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| Synonyms |
IRAK4IN28; IRAK4-IN-28; IRAK4 inhibitor 28
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| HS Tariff Code |
2934.99.9001
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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 : ~10 mg/mL (~25.94 mM)
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|---|---|
| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 1 mg/mL (2.59 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 10.0 mg/mL clear DMSO stock solution to 400 μL of PEG300 and mix evenly; then add 50 μL of Tween-80 to the above solution and mix evenly; then add 450 μL of 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 mg/mL (2.59 mM) (saturation unknown) in 10% DMSO + 90% (20% SBE-β-CD in 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 10.0 mg/mL clear DMSO stock solution to 900 μL of 20% SBE-β-CD physiological saline solution and mix evenly. Preparation of 20% SBE-β-CD in Saline (4°C，1 week): Dissolve 2 g SBE-β-CD in 10 mL saline to obtain a clear solution. View More
Solubility in Formulation 3: ≥ 1 mg/mL (2.59 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one), clear solution. |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 2.5940 mL | 12.9702 mL | 25.9403 mL | |
| 5 mM | 0.5188 mL | 2.5940 mL | 5.1881 mL | |
| 10 mM | 0.2594 mL | 1.2970 mL | 2.5940 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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