产品说明书

AZ1495

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Chemical Structure| 2196204-23-4 同义名 : -
CAS号 : 2196204-23-4
货号 : A1157106
分子式 : C21H31N5O2
纯度 : 97%
分子量 : 385.503
MDL号 : MFCD31813626
存储条件：

粉末 Keep in dark place,Sealed in dry,2-8°C

液体 -20°C:3-6个月-80°C:12个月
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：
生物活性
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].
实验方案
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
参考文献

[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.