AZ1495，一种弱碱，是一种有效的白细胞介素-1 受体相关激酶 4 (IRAK4) 抑制剂，具有口服活性。AZ1495 对 IRAK4 和 IRAK1 具有良好的理化和激酶选择性，其 IC₅₀ 值分别为 0.005 μM 和 0.023 μM。AZ1495 具有 IRAK4 抑制作用，K_d 值为 0.0007 μM。AZ1495 可用于弥漫大 B 细胞淋巴瘤 (DLBCL) 的研究。

AZ1495, a weak base, is a potent orally active interleukin-1 receptor associated kinase 4 (IRAK4) inhibitor. AZ1495 has a favorable physicochemical and kinase selectivity for IRAK4 and IRAK1 with IC 50 values of 0.005 μM and 0.023 μM, respectively. AZ1495 has IRAK4 inhibition with a K d value of 0.0007 μM. AZ1495 can be used for the research of diffuse large B-cell lymphoma (DLBCL).

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IRAK4 5 nM (IC50) IRAK1 23 nM (IC50

AZ1495 (compound 28) (10 μM,1 h) has kinase selectivity for IRAK4 with IC50 values of 0.005 μM (enzyme assay) and 0.052 μM (cellular assay), respectively.
AZ1495 (10 μM,1 h) has kinase inhibition for IRAK4 with an IC50 value of 0.005 μM and Kd value of 0.0007 μM.
AZ1495 (0.001-100 μM, 72 h) inhibits NF-κB activation and growth of ABC-DLBCL cell lines in a dosedependent manner.
AZ1495 (0-3.3 μM, 14 h) completely inhibits NF-κB signaling and induces cell death at lower concentration in combination with a BTK inhibitor in OCI-LY10 cells. has not independently confirmed the accuracy of these methods. They are for reference only.

AZ1495 (compound 28) (oral, daily, 12.5 mg/kg) leds to tumor regression combination with ibrutinib in an ABC-DLBCL mouse model (OCI-LY10 cells).
AZ1495 (iv., 2 mg/kg and oral, 5mg/kg) is characterized by high clearance (Cl) in rat (75 mL/min/kg) and moderate predictions based on hepatocyte data (Clint 15 μl/min/106 cells, predicted clearance 42 mL/min/kg) with low bioavailability consistent with a high first pass effect.
AZ1495 (iv., 1 mg/kg) has low the amount of active renal secretion occurring in the dog. has not independently confirmed the accuracy of these methods. They are for reference only.

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[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.

In Vitro: DMSO : 10 mg/mL (25.94 mM; Need ultrasonic)配制储备液