化合物CNX-774 T2302

Product Introduction
Bioactivity


英文名: CNX-774

描述: CNX-774 是一种选择性的、具有口服活性的、不可逆的 BTK 抑制剂 (IC50<1 nM)。它能够特异性靶向 Btk 的 Cys 481进行共价修饰。

激酶实验: In vitro kinase assays: The p38α and p38β are assayed in 25 mM Tris-HCl, pH 7.5, containing 0.1 mM EGTA, with myelin basic protein (0.33 mg/mL) as substrate. Assays are performed either manually for 10 minutes at 30 °C in 50 μL incubations using [γ-33P]ATP, or with a Biomek 2000 Laboratory Automation Workstation in a 96-well format for 40 minutes at ambient temperature in 25 μL incubations using [γ-33P]ATP. The concentrations of ATP and magnesium acetate are 0.1 mM and 10 mM respectively. All assays are initiated with MgATP. Manual assays are terminated by spotting aliquots of incubation on to phosphocellulose paper, followed by immersion in 50 mM phosphoric acid. Robotic assays are terminated by the addition of 5 μL of 0.5 M phosphoric acid before spotting aliquots on to P30 filter mats. All papers are then washed four times in 50 mM phosphoric acid to remove ATP, once in acetone (manual incubations) or methanol (robotic incubations), and then dried and counted for radioactivity.

体内活性: 在细胞试验中,CNX-774以BTK的ATP结合位点Cys-481残基为靶点从而抑制其活性（IC50：1-10 nM）。

存储条件: Powder: -20°C for 3 years | In solvent: -80°C for 1 year

溶解度: Ethanol : 2 mg/mL (4.0 mM)
H2O : < 1 mg/mL (insoluble or slightly soluble)
DMSO : 93 mg/mL (186.2 mM)


关键字: Bruton tyrosine kinase | Btk | CNX-774 | B-cell | BCR | Inhibitor | inhibit | CNX774 | autoimmune

相关产品: JAK3/BTK-IN-2 | ONO-4059 analog | Cinsebrutinib | BMS-986142 | ACP-5862 | RN486 | BMS-935177 | PCI-33380 | BTK IN-1 | BTK inhibitor 1

相关库: Cysteine Covalent Library | Angiogenesis related Compound Library | Immuno-Oncology Compound Library | Fluorochemical Library | Kinase Inhibitor Library | Inhibitor Library | Highly Selective Inhibitor Library | Tyrosine Kinase Inhibitor Library | Orally Active Compound Library | Covalent Inhibitor Library

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注：该产品未在中华人民共和国食品药品监督管理部门申请医疗器械注册和备案，不可用于临床诊断或治疗等相关用途