化合物 Spebrutinib|T2603

Spebrutinib
1202757-89-8

￥498 5mg 起订

￥747 10mg 起订

￥2161 50mg 起订

上海更新日期：2024-09-14

TargetMol中国（陶术生物）

VIP12年

联系人：邵小姐

电话：021-021-33632979拨打

手机：15002134094 拨打

邮箱：marketing@targetmol.com

产品详情:

中文名称：: 化合物 Spebrutinib

英文名称：: Spebrutinib

CAS号：: 1202757-89-8

品牌：: TargetMol

产地：: 美国

保存条件：: Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice.

纯度规格：: 97.02%

产品类别：: 抑制剂

货号：: T2603

Product Introduction

Bioactivity

Name	Spebrutinib
Description	Spebrutinib (LMK-435) is an orally bioavailable, selective inhibitor of Bruton's agammaglobulinemia tyrosine kinase (BTK), with potential antineoplastic activity.
Cell Research	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)
Kinase Assay	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.
In vitro	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.
In vivo	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。
Storage	Powder: -20°C for 3 years \| In solvent: -80°C for 1 year \| Shipping with blue ice.
Solubility Information	Ethanol : < 1 mg/mL (insoluble or slightly soluble) DMSO : 79 mg/mL (186.6 mM) H2O : < 1 mg/mL (insoluble or slightly soluble)
Keywords	Spebrutinib \| inhibit \| Bruton tyrosine kinase \| CC 292 \| Btk \| AVL 292 \| CC292 \| Inhibitor \| LMK 435 \| AVL292 \| LMK435
Inhibitors Related	Pelitinib \| Ponatinib \| IBT6A \| SI-2 hydrochloride \| Vemurafenib \| Bosutinib hydrate \| Staurosporine \| Nintedanib \| Dasatinib \| (±)-Zanubrutinib \| Ibrutinib \| Orelabrutinib
Related Compound Libraries	Inhibitor Library \| Bioactive Compound Library \| Anti-Cancer Active Compound Library \| Bioactive Compounds Library Max \| Kinase Inhibitor Library \| Highly Selective Inhibitor Library \| Drug Repurposing Compound Library \| Tyrosine Kinase Inhibitor Library \| Anti-Cancer Clinical Compound Library \| Anti-Cancer Drug Library

LMK-435|||CC-292|||AVL-292|TargetMol

上海陶术生物科技有限公司为美国Target Molecule Corp. ( Target Mol ) 在上海建立的全资子公司。我们与美国波士顿、德国慕尼黑的同事一起，为北美、欧洲和亚洲从事药物研发和生物学研究的科学家提供优质的产品和专业的服务。公司下设筛选事业部，化学事业部，生物事业部和新材料部。从虚拟筛选到实体化合物分子供应；从商业化产品销售到个性化定制合成；从对明确靶点的分子筛选到对明确分子的多靶点筛选，从高通量筛选到化学结构优化，我们都可以满足您的科研用品及技术服务的需求。经过在中国市场五年的精心耕耘，我们已成为筛选化合物领域优秀的供应商，为超过五百家学校和各类企业提供了品质卓越的小分子化合物和药物筛

成立日期	(12年)
注册资本	566.2651万人民币
员工人数	100-500人
年营业额	￥ 1亿以上
经营模式	贸易,试剂,定制,服务
主营行业	化学试剂,生物活性小分子