AZ1495 是一种弱碱性、口服活性有效的白细胞介素-1 受体相关激酶 4 (IRAK4) 抑制剂。AZ1495 对 IRAK4 和 IRAK1 具有良好的物理化学和激酶选择性,IC50 值分别为 0.005 μM 和 0.023 μM。
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描述 | AZ1495 is a potent, orally active inhibitor of IRAK4. AZ1495 has good physicochemical and kinase selectivity for IRAK4 and IRAK1, with IC50 values of 0.005 μM and 0.023 μM, respectively. The Kd value for IRAK4 inhibition by AZ1495 is 0.0007 μM. AZ1495 inhibits IRAK4 with a Kd value of 0.0007 μM in the concentration range of 0.001-100 μM. In the range of 0.001-100 μM, AZ1495 inhibited NF-κB activation and the growth of ABC-DLBCL cell line in a dose-dependent manner for 72 hours. At concentrations less than 3.3 μM for 14 hours, AZ1495 completely inhibited NF-κB signalling, and at lower concentrations in combination with BTK inhibitors induced OCI-LY10 cell death[1]. |
Animal study | In an ABC-DLBCL mouse model (OCI-LY10 cells), AZ1495 demonstrated modest anti-tumour activity when administered orally daily at a dose of 12.5 mg/kg. When combined with Ibrutinib, it resulted in tumour regression[1]. |
计算器 | ||||
存储液制备 | 1mg | 5mg | 10mg | |
1 mM 5 mM 10 mM |
2.59mL 0.52mL 0.26mL |
12.97mL 2.59mL 1.30mL |
25.94mL 5.19mL 2.59mL |
CAS号 | 2196204-23-4 |
分子式 | C21H31N5O2 |
分子量 | 385.503 |
别名 | |
运输 | 蓝冰 |
存储条件 |
液体 -20°C:3-6个月-80°C:12个月 粉末 Keep in dark place,Sealed in dry,2-8°C |
溶解度 |
DMSO: 9 mg/mL(23.35 mM),配合低频超声助溶,注意:DMSO长时间开封后,会吸水并导致溶解能力下降,请避免使用长期开封的DMSO |
动物实验配方 |