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- 保存条件：
Powder: -20°C, 3 years; 4°C, 2 years.In solvent: -80°C, 6 months; -20°C, 1 month.
- 库存：
货期：1-2天
- 供应商：
MedChemExpress LLC
- CAS号：
2196204-23-4
- 规格：
10 mM * 1 mL/1 mg/5 mg/10 mg
| 规格： | 10 mM * 1 mL | 产品价格： | ￥2073.0 |
|---|---|---|---|
| 规格： | 1 mg | 产品价格： | ￥1160.0 |
| 规格： | 5 mg | 产品价格： | ￥2444.0 |
| 规格： | 10 mg | 产品价格： | ￥3910.0 |
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AZ1495
CAS No. : 2196204-23-4
MCE 国际站：AZ1495
产品活性：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，Kd 值为 0.0007 μM。AZ1495 可用于弥漫大 B 细胞淋巴瘤 (DLBCL) 的研究。
作用靶点：IRAK
In Vitro: 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.
In Vivo: 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.
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文献和实验Assessment of Drug Transporter Function Using Fluorescent Cell Imaging
Figure 23.6.1 Distribution of fluorescent substrate (FS) solution and medium in preparation for the addition of positive control inhibitor and various concentrations of test inhibitors in subsequent steps
protein folding as a basis of human disease. Trends in Biochem Sci, 1995, 20(11): 457～459 [23] Taubes G. Misfolding the way to disease. Science, 1996, 271(5255): 1493～1495 [24] Baker D, Agard D. Kinetics versus thermodynamics in protein folding
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