AZ1495是一种新型的、具有口服活性的白细胞介素-1受体相关激酶4（IRAK4）抑制剂。
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.
AZ1495是一种新型的、具有口服活性的白细胞介素-1受体相关激酶4（IRAK4）抑制剂。AZ1495可抑制IRAK4（IC50=5nM）和IRAK1（IC50=23nM）的活性。AZ1495可用于弥漫性大B细胞淋巴瘤（DLBCL）的相关研究[1-2]。
在体外，AZ1495（1μM）处理高渗环境下的人角膜上皮细胞（HCECs）24小时，显著抑制了IRAK1蛋白的表达及其下游炎症因子和凋亡因子的表达，并增强了细胞活力[1]。AZ1495（1nM-100μM）处理OCI-LY10细胞3天，能有效抑制NF-κB通路的激活（如降低p-IκBα水平），并诱导细胞死亡[2]。
在体内，在OCI-LY10异种移植瘤小鼠模型中，AZ1495（12.5mg/kg；每日一次口服给药；连续处理51天）单独处理，能够抑制肿瘤生长抑制；当AZ1495与Ibrutinib（12mg/kg；每日一次口服给药）联合使用时，能够导致肿瘤消退[2]。
| 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 | ||
| 分子式 | C21H31N5O2 | 分子量 | 385.5 |
| 溶解度 | DMSO : 10 mg/mL (25.94 mM) | 储存条件 | Store at -20°C |
| General tips | 请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液；一旦配成溶液，请分装保存，避免反复冻融造成的产品失效。 储备液的保存方式和期限：-80°C 储存时，请在 6 个月内使用，-20°C 储存时，请在 1 个月内使用。 为了提高溶解度，请将管子加热至37℃，然后在超声波浴中震荡一段时间。 |
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| Shipping Condition | 评估样品解决方案：配备蓝冰进行发货。所有其他可用尺寸：配备RT，或根据请求配备蓝冰。 | ||
| 制备储备液 | |||
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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 |
| 第一步：请输入基本实验信息（考虑到实验过程中的损耗，建议多配一只动物的药量） | ||||||||||
| 给药剂量 | mg/kg |  |
动物平均体重 | g | |
每只动物给药体积 | ul | |
动物数量 | 只 |
| 第二步：请输入动物体内配方组成（配方适用于不溶于水的药物；不同批次药物配方比例不同，请联系GLPBIO为您提供正确的澄清溶液配方） | ||||||||||
| % DMSO % % Tween 80 % saline | ||||||||||
| 计算重置 | ||||||||||
计算结果:
工作液浓度： mg/ml；
DMSO母液配制方法： mg 药物溶于 μL DMSO溶液（母液浓度 mg/mL，
体内配方配制方法：取 μL DMSO母液，加入 μL PEG300，混匀澄清后加入μL Tween 80，混匀澄清后加入 μL saline，混匀澄清。
1. 首先保证母液是澄清的；
2.
一定要按照顺序依次将溶剂加入，进行下一步操作之前必须保证上一步操作得到的是澄清的溶液，可采用涡旋、超声或水浴加热等物理方法助溶。
3. 以上所有助溶剂都可在 GlpBio 网站选购。
Quality Control & SDS
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- Purity: >99.50% Appearance: A solid
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