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Pack Size | Price | Availability | Quantity |
---|---|---|---|
5 mg | $43 | In Stock | |
10 mg | $67 | In Stock | |
25 mg | $92 | In Stock | |
50 mg | $117 | In Stock | |
100 mg | $147 | In Stock | |
200 mg | $198 | In Stock | |
500 mg | $328 | In Stock | |
1 mL x 10 mM (in DMSO) | $63 | In Stock |
Description | Baricitinib (INCB028050) is an orally bioavailable inhibitor of Janus kinases 1 and 2 (JAK1/2), with potential anti-inflammatory, immunomodulating and antineoplastic activities. |
In vitro | In adjuvant-induced arthritis rat models, Baricitinib (10 mg/kg orally) inhibits JAK1/2 signaling pathways and suppresses immune infiltration. In both CIA and CAIA models, Baricitinib (10 mg/kg) mitigates cartilage damage and inflammation and inhibits delayed-type hypersensitivity reactions. |
In vivo | In immature T cells isolated from the peripheral blood (IC50=20 nM), Baricitinib inhibits the phosphorylation of STAT3 stimulated by IL-23. Additionally, in peripheral blood mononuclear cells, Baricitinib suppresses the phosphorylation of the STAT3 substrate induced by IL-6 (IC50=44 nM) and subsequently inhibits the production of the chemokine MCP-1 (IC50=40 nM). |
Kinase Assay | 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]. |
Cell Research | 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]. |
Alias | INCB028050, LY3009104 |
Molecular Weight | 371.42 |
Formula | C16H17N7O2S |
Cas No. | 1187594-09-7 |
Storage | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | ||||||||||||||||||||||||||||||||||||||||
Solubility Information | 5% DMSO+95% Saline: 3.45 mg/mL (9.29 mM, precipitation) ![]() H2O: < 1 mg/mL (insoluble or slightly soluble) Ethanol: < 1 mg/mL (insoluble or slightly soluble) DMSO: 55 mg/mL (148.08 mM) ![]() | ||||||||||||||||||||||||||||||||||||||||
Solution Preparation Table | |||||||||||||||||||||||||||||||||||||||||
DMSO/5% DMSO+95% Saline
DMSO
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