巴瑞克替尼 T2485

Product Introduction
Bioactivity


英文名: Baricitinib

描述: Baricitinib (INCB028050) 是一种选择性，可口服的JAK1和JAK2抑制剂，IC50分别为5.9 nM 和 5.7 nM，具有潜在的抗炎、免疫调节和抗肿瘤活性。

细胞实验: Baricitinib(INCB 028050) is dissolved in stock solutions, and then diluted with appropriate media before use[1]. Human PBMCs are isolated by leukapheresis followed by Ficoll-Hypaque centrifugation. For the determination of IL-6-induced MCP-1 production, PBMCs are plated at 3.3×105 cells per well in RPMI 1640+10% FCS in the presence or absence of various concentrations of INCB028050 (1 nM, 10 nM, 100 nM, 1 μM, and 10 μM). Following preincubation with compound for 10 min at room temperature, cells are stimulated by adding 10 ng/mL human recombinant IL-6 to each well. Cells are incubated for 48 h at 37°C, 5% CO2. Supernatants are harvested and analyzed by ELISA for levels of human MCP-1. The ability of INCB028050 to inhibit IL-6-induced secretion of MCP-1 is reported as the concentration required for 50% inhibition (IC50). Proliferation of Ba/F3-TEL-JAK3 cells is performed over 3 d using Cell-Titer Glo[1].

激酶实验: Enzyme assays are performed using a homogeneous time-resolved fluorescence assay with recombinant epitope tagged kinase domains (JAK1, 837-1142; JAK2, 828-1132; JAK3, 718-1124; Tyk2, 873-1187) or full-length enzyme (cMET and Chk2) and peptide substrate. Each enzyme reaction is performed with or without test compound (11-point dilution), JAK, cMET, or Chk2 enzyme, 500 nM (100 nM for Chk2) peptide, ATP (at the Km specific for each kinase or 1 mM), and 2.0% DMSO in assay buffer. The calculated IC50 value is the compound concentration required for inhibition of 50% of the fluorescent signal. Additional kinase assays are performed at Cerep using standard conditions at 200 nM. Enzymes tested included: Abl, Akt1, AurA, AurB, CDC2, CDK2, CDK4, CHK2, c-kit, EGFR, EphB4, ERK1, ERK2, FLT-1, HER2, IGF1R, IKKα, IKKβ, JNK1, Lck, MEK1, p38α, p70S6K, PKA, PKCα, Src, and ZAP70[1].

体外活性: 在佐剂性关节炎大鼠模型中Baricitinib（10 mg / kg口服）可抑制JAK1 / 2信号传导,同时抑制免疫浸润.在CIA和CAIA模型中,Baricitinib（10 mg / kg）改善软骨损伤和炎症,抑制迟发型超敏反应.

体内活性: 在分离的未成熟型T 细胞中（IC50=20 nM）,Baricitinib抑制IL-23刺激的STAT3的磷酸化。在外周血单核细胞中,Baricitinib抑制IL-6刺激底物STAT3的磷酸化（IC50=44 nM）以及随后趋化因子MCP-1（IC50=40 nM）的产生。

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

溶解度: 5% DMSO+95% Saline : 3.45 mg/mL (9.29 mM, suspension)
H2O : < 1 mg/mL (insoluble or slightly soluble)
Ethanol : < 1 mg/mL (insoluble or slightly soluble)
DMSO : 55 mg/mL (148.08 mM)


关键字: Inhibitor | JAK | Janus kinase | INCB-028050 | inhibit | Baricitinib | LY 3009104 | INCB 028050 | LY-3009104

相关产品: Oclacitinib maleate | PP2 | Ilginatinib maleate | Deucravacitinib | Filgotinib | JAK-IN-21 | Brepocitinib | NVP-BSK805 2HCl (1092499-93-8(free base)) | Larotinib | Decernotinib

相关库: Drug Repurposing Compound Library | FDA-Approved Kinase Inhibitor Library | Anti-Cancer Drug Library | Kinase Inhibitor Library | Anti-Cancer Clinical Compound Library | Inhibitor Library | Anti-Cancer Approved Drug Library | Tyrosine Kinase Inhibitor Library | Anti-Cancer Active Compound Library | EMA Approved Drug 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