AZ1495 是一种弱碱,是一种有效的口服活性白细胞介素 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。 AZ1495 具有 IRAK4 抑制作用,Kd 值为 0.0007 μM。 AZ1495可用于弥漫性大B细胞淋巴瘤(DLBCL)的研究。
Cas No. | 2196204-23-4 |
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 | For obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while. |
Shipping Condition | Evaluation sample solution : ship with blue ice All other available size: ship with RT , or blue ice upon request |
产品描述 | AZ1495 (compound 28) is an oral active inhibitor of Interleukin-1 receptor associated kinase 4 (IRAK4), with IC50 values of 5 nM and 23 nM for IRAK4 and IRAK1, respectively. Shows activity in treatment of mutant MYD88L265P diffuse large B-cell lymphoma (DLBCL)[1]. [1]. Scott JS, 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. |