Powder: -20°C for 3 years | In solvent: -80°C for 1 year
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。
规格 | 价格/CNY | 货期 | 数量 | |
---|---|---|---|---|
1 mg | ¥ 329 | 现货 | ||
2 mg | ¥ 472 | 现货 | ||
5 mg | ¥ 932 | 现货 | ||
10 mg | ¥ 1,320 | 现货 | ||
25 mg | ¥ 1,960 | 现货 | ||
50 mg | ¥ 2,730 | 现货 | ||
100 mg | ¥ 4,320 | 现货 | ||
200 mg | ¥ 6,120 | 现货 | ||
500 mg | ¥ 8,900 | 现货 | ||
1 g | ¥ 12,200 | 现货 | ||
1 mL * 10 mM (in DMSO) | ¥ 813 | 现货 |
产品描述 | Baricitinib (INCB028050) is an orally bioavailable inhibitor of Janus kinases 1 and 2 (JAK1/2), with potential anti-inflammatory, immunomodulating and antineoplastic activities. |
靶点活性 | JAK2:5.7 nM, JAK1:5.9 nM, TYK2:53 nM, JAK3:>400 nM |
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。 |
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]. |
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]. |
别名 | INCB028050, LY3009104, 巴瑞克替尼 |
化合物与蛋白结合的复合物 |
Crystal Structure of BMP-2-inducible kinase in complex with baricitinib |
分子量 | 371.42 |
分子式 | C16H17N7O2S |
CAS No. | 1187594-09-7 |
Powder: -20°C for 3 years | In solvent: -80°C for 1 year
H2O: < 1 mg/mL (insoluble or slightly soluble)
Ethanol: < 1 mg/mL (insoluble or slightly soluble)
DMSO: 69 mg/mL (185.8 mM)
可选溶剂 | 浓度 体积 质量 | 1 mg | 5 mg | 10 mg | 25 mg |
DMSO | 1 mM | 2.6924 mL | 13.4618 mL | 26.9237 mL | 67.3092 mL |
5 mM | 0.5385 mL | 2.6924 mL | 5.3847 mL | 13.4618 mL | |
10 mM | 0.2692 mL | 1.3462 mL | 2.6924 mL | 6.7309 mL | |
20 mM | 0.1346 mL | 0.6731 mL | 1.3462 mL | 3.3655 mL | |
50 mM | 0.0538 mL | 0.2692 mL | 0.5385 mL | 1.3462 mL | |
100 mM | 0.0269 mL | 0.1346 mL | 0.2692 mL | 0.6731 mL |
对于不同动物的给药剂量换算,您也可以参考 更多...
请在以下方框中输入您的动物实验信息后点击计算,可以得到母液配置方法和体内配方的制备方法: 比如您的给药剂量是10 mg/kg,每只动物体重20 g,给药体积100 μL,一共给药动物10 只,您使用的配方为5% DMSO+30% PEG300+5% Tween 80+60% ddH2O。那么您的工作液浓度为2 mg/mL。
母液配置方法:2 mg 药物溶于 50 μL DMSO (母液浓度为 40 mg/mL), 如您需要配置的浓度超过该产品的溶解度,请先与我们联系。
体内配方的制备方法:取 50 μL DMSO 主液,加入 300 μL PEG300, 混匀澄清,再加 50 μL Tween 80,混匀澄清,再加 600 μL ddH2O, 混匀澄清。
您可能有的问题的答案可以在抑制剂处理说明中找到,包括如何准备库存溶液,如何存储产品,以及基于细胞的分析和动物实验需要特别注意的问题。
Baricitinib 1187594-09-7 Angiogenesis Cell Cycle/Checkpoint Chromatin/Epigenetic JAK/STAT signaling Stem Cells Tyrosine Kinase/Adaptors Tyrosine Kinases JAK Chk Inhibitor INCB028050 Janus kinase INCB-028050 LY3009104 巴瑞克替尼 inhibit LY 3009104 INCB 028050 LY-3009104 inhibitor