Spebrutinib
作者：齐岳
发布时间：2023-08-23
09:17:12
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产品名称：Spebrutinib
产品描述：
| 产品描述 | Spebrutinib is an orally bioavailable, selective inhibitor of Bruton's agammaglobulinemia tyrosine kinase (BTK), with potential antineoplastic activity. |
| 靶点活性 | BTK:<0.5 nM |
| 体外活性 | 口服3-30 mg/kg AVL-292抑制胶原蛋白诱导的小鼠关节炎模型中的炎症临床症状,包括关节和爪肿胀以及感染爪的可见发红的减少. |
| 体内活性 | AVL-292通过抑制BTK的活性,进一步抑制B细胞的增殖,EC50为3 nM。AVL-29对在Ramos细胞中的BTK产生抑制作用,EC50为8 nM,具有剂量依赖性,并且抑制了下游的BCR通路。 |
| 激酶实验 | Procedures for BTK OMNIA Assay: The Omnia continuous read assay is performed essentially as described by the vendor. The assay conditions are: 40 μM ATP (1X KMATP), 10 μM Y5-Sox, and 10 nM BTK enzyme. Briefly, a substrate mix containing 1.13X ATP and the Y5 Sox substrate is first prepared in 1X Omnia Kinase Reaction Buffer (KRB) consisting of 20 mM Tris, pH 7.5, 5 mM MgCl2, 1 mM EGTA, 5 mM?β-glycerophosphate, 5% glycerol, and 0.2 mM DTT. For IC50 measurements, 5 μL of enzyme are incubated with serially diluted (3-fold) compounds prepared in 50% DMSO in a Corning (#3574) 384-well, white, non-binding surface microtiter plate at 25°C for 30 min. Kinase reactions are started with the addition of 45 μL of the ATP/Y5 substrate mix and monitored at λex360/λem485 in a Synergy 4 plate reader for 60 minutes. Progress curves from each well are examined for linear reaction kinetics and fit statistics. Initial velocity from each reaction is determined from the slope of a plot of relative fluorescence units versus time and then plotted against inhibitor concentration to estimate IC50 using the Response, Variable Slope model in GraphPad Prism from GraphPad Software. |
| 细胞实验 | A suspension of resting purified na?ve human B cells isolated by negative selection in RPMI is prepared at 0.4–0.5 × 106 cells/ml. Cells are mixed together with α-human IgM (final concentration of 5 μg/ml in each well) and vehicle (dimethyl sulfoxide) or AVL-292 (final concentrations of 0.01, 0.1, 1.0, 10.0, 100.0, or 1000 nM per well) and seeded in a 96-well plate. Cells are incubated for 56 hours in a humidified incubator maintained at 37°C and 5% CO2. 3H-Thymidine is added (final concentration of 1 μCi in each well) and cells are incubated overnight, harvested, and measured for 3H incorporation. Experiments are performed in triplicate.(Only for Reference) |
| 别名 | AVL-292, LMK-435, CC-292 |
| 分子量 | 423.448 |
| 分子式 | C22H22FN5O3 |
| CAS No. | 1202757-89-8 |
存储
Powder: -20°C for 3 years | In solvent: -80°C for 2 years
溶解度
Ethanol: <1 mg/mL
DMSO: 79 mg/mL (186.6 mM)
H2O: <1 mg/mL
( < 1 mg/mL refers to the product slightly soluble or insoluble )
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