AZ1495 |
Catalog No.GC33054
One-Click Copy Product Info
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AZ1495, una base débil, es un potente inhibidor de la quinasa 4 asociada al receptor de la interleucina-1 activo por vÍa oral (IRAK4). AZ1495 tiene una selectividad fisicoquÍmica y quinasa favorable para IRAK4 e IRAK1 con valores de CI50 de 0,005 μM y 0,023 μM, respectivamente. AZ1495 tiene una inhibiciÓn de IRAK4 con un valor de Kd de 0,0007 μM. AZ1495 se puede utilizar para la investigaciÓn del linfoma difuso de células B grandes (DLBCL).
Products are for research use only. Not for human use. We do not sell to patients.
Cas No.: 2196204-23-4
Sample solution is provided at 25 µL, 10mM.
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AZ1495 is a novel, orally active interleukin-1 receptor-associated kinase 4 (IRAK4) inhibitor. AZ1495 inhibits the activity of both IRAK4 (IC50=5nM) and IRAK1 (IC50=23nM). AZ1495 can be used in research related to diffuse large B-cell lymphoma (DLBCL)[1-2].
In vitro, AZ1495 (1μM) was used to treat human corneal epithelial cells (HCECs) under hypertonic conditions for 24 hours. AZ1495 significantly inhibited the expression of the IRAK1 protein and its downstream inflammatory and apoptotic factors, and enhanced cell viability[1]. AZ1495 (1nM-100μM) was used to treat OCI-LY10 cells for 3 days, effectively inhibiting the activation of the NF-κB pathway (e.g., by reducing p-IκBα levels) and inducing cell death[2].
In vivo, in an OCI-LY10 xenograft mouse model, AZ1495 (12.5mg/kg; administered orally once daily; for 51 consecutive days) alone was shown to inhibit tumor growth. When AZ1495 was combined with Ibrutinib (12mg/kg; administered orally once daily), AZ1495 led to tumor regression[2].
References:
[1] Liu Y, Jiang Y, Song C, et al. The role of miR-146a/IRAK1/JNK1 pathway in mediating the effects of Yiqi Congming decoction on dry eye: A mechanistic study in rat models. J Ethnopharmacol. 2025 May 12;347:119698.
[2] Scott JS, Degorce SL, Anjum R, et al. Discovery and Optimization of Pyrrolopyrimidine Inhibitors of Interleukin-1 Receptor Associated Kinase 4 (IRAK4) for the Treatment of Mutant MYD88L265P Diffuse Large B-Cell Lymphoma. J Med Chem. 2017 Dec 28;60(24):10071-10091.
| Cell experiment [1]: | |
Cell lines | Human corneal epithelial cells (HCECs) |
Preparation Method | HCECs were cultured in Endothelial Cell Medium (ECM) supplemented with 5% FBS and AZ1495 (1μM). |
Reaction Conditions | 1μM; 24 hours. |
Applications | AZ1495 enhanced the proliferative activity (cell viability) of HCECs under hyperosmolarity-induced stress. AZ1495 significantly inhibited the hyperosmotic saline-induced activation of the IRAK1-JNK1 pathway and the expression of pro-inflammatory cytokines (e.g., MMP-9, TNF-α, IL-1β, Caspase-3, IL-6, IFN-γ) at both mRNA and protein levels. |
| Animal experiment [2]: | |
Animal models | Female CB.17 SCID mice bearing OCI-LY10 (ABC-DLBCL) tumor xenografts. |
Preparation Method | In the OCI-LY10 xenograft mouse model, AZ1495 (12.5mg/kg) administered orally once daily for 51days. |
Dosage form | 12.5mg/kg; p.o.; Daily oral administration. |
Applications | AZ1495 led to a 60% tumor growth inhibition. When administered in combination with the BTK inhibitor Ibrutinib (12mg/kg; p.o.), the treatment led to tumor regression, demonstrating a synergistic antitumor effect in the mutant MYD88L265P DLBCL model. |
References: | |
| Cas No. | 2196204-23-4 | SDF | |
| Canonical SMILES | C1(C(C2CCOCC2)=CN3)=C3N=CN=C1N[C@@H]4CC[C@@H](N5CCOCC5)CC4 | ||
| Formula | C21H31N5O2 | M.Wt | 385.5 |
| Solubility | DMSO : 10 mg/mL (25.94 mM) | 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 | 2.594 mL | 12.9702 mL | 25.9403 mL |
| 5 mM | 518.8 μL | 2.594 mL | 5.1881 mL |
| 10 mM | 259.4 μL | 1.297 mL | 2.594 mL |
Step 1: Enter information below (Recommended: An additional animal making an allowance for loss during the experiment)
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μL
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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 saline, 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.
Quality Control & SDS
- View current batch:
- Purity: >99.50% Appearance: A solid
- COA (Certificate of Analysis)
- SDS (Safety Data Sheet)
- Datasheet
Average Rating: 5 (Based on Reviews and 30 reference(s) in Google Scholar.)