Baricitinib [1187594-09-7]
Cat# T2485-1mL
Size : 1mL
Brand : TargetMol
Baricitinib
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Purity:100%
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COA HPLC HNMR
Baricitinib
Catalog No. T2485Cas No. 1187594-09-7
Baricitinib (INCB028050) is an orally bioavailable inhibitor of Janus kinases 1 and 2 (JAK1/2), with potential anti-inflammatory, immunomodulating and antineoplastic activities.
All TargetMol products are for research purposes only and cannot be used for human consumption. We do not provide products or services to individuals. Please comply with the intended use and do not use TargetMol products for any other purpose. Pack Size | |
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5 mg | |
10 mg | |
25 mg | |
50 mg | |
100 mg | |
200 mg | |
500 mg | |
1 mL x 10 mM (in DMSO) |
Product Introduction
Bioactivity
Chemical Properties
Storage & Solubility Information
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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Calculator
In Vivo Formulation Calculator (Clear solution)
Please enter your animal experiment information in the following box and click Calculate to obtain the mother liquor preparation method and in vivo formula preparation method:
For example, your dosage is 10 mg/kg Each animal weighs 20 g, and the dosage volume is 100 μL . A total of 10 animals were administered, and the formula you used is 5% DMSO+30% PEG300+5% Tween 80+60% ddH2O. So your working solution concentration is 2 mg/mL。
Mother liquor preparation method: 2 mg of drug dissolved in 50 μL DMSO (mother liquor concentration of 40 mg/mL), if you need to configure a concentration that exceeds the solubility of the product, please contact us first.
Preparation method for in vivo formula: Take 50 μL DMSO main solution, add 300 μLPEG300 mix well and clarify, then add 50 more μL Tween 80, mix well and clarify, then add 600 more μLddH2O mix well and clarify
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Tech Support
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Keywords
InhibitorJAKJanus kinaseINCB-028050inhibitBaricitinibLY 3009104INCB 028050LY-3009104