Powder: -20°C for 3 years | In solvent: -80°C for 1 year
Baricitinib [1187594-09-7]
Katalog-Nummer T2485-25mg
Size : 25mg
Marke : TargetMol
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Baricitinib
Catalog No. T2485 CAS 1187594-09-7
Synonyms: INCB028050, LY3009104
Baricitinib (INCB028050) is an orally bioavailable inhibitor of Janus kinases 1 and 2 (JAK1/2), with potential anti-inflammatory, immunomodulating and antineoplastic activities.
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Baricitinib, CAS 1187594-09-7
| Description | Baricitinib (INCB028050) is an orally bioavailable inhibitor of Janus kinases 1 and 2 (JAK1/2), with potential anti-inflammatory, immunomodulating and antineoplastic activities. |
| Targets&IC50 | JAK2:5.7 nM, JAK1:5.9 nM, TYK2:53 nM, JAK3:>400 nM |
| 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]. |
| Synonyms | INCB028050, LY3009104 |
| Molecular Weight | 371.42 |
| Formula | C16H17N7O2S |
| CAS No. | 1187594-09-7 |
Storage
Solubility Information
H2O: < 1 mg/mL (insoluble or slightly soluble)
Ethanol: < 1 mg/mL (insoluble or slightly soluble)
DMSO: 69 mg/mL (185.8 mM)
References and Literature
1. Fridman JS, et al. J Immunol, 2010, 184(9), 5298-5307. 2. Kontzias A, et al. Curr Opin Pharmacol, 2012, 12(4), 464-470. 3. Norman P, et al. Expert Opin Ther Pat, 2012, 22(10), 1233-1249. 4. Norman P, et al. Expert Opin Ther Pat, 2012, 22(9), 1105-1109. 5. Kvacskay P, Yao N, Schnotz J H, et al. Increase of aerobic glycolysis mediated by activated T helper cells drives synovial fibroblasts towards an inflammatory phenotype: new targets for therapy?[J]. Arthritis Research & Therapy. 2021, 23(1): 1-15.
Citations
1. Si H, Wang J, He R, et al. Identification of U937JAK3-M511I Acute Myeloid Leukemia Cells as a Sensitive Model to JAK3 Inhibitor. Frontiers in oncology. 2021, 11: 807200-807200. 2. Yao N, Tretter T, Kvacskay P, et al. Targeting of Janus Kinases Limits Pro-Inflammatory but Also Immunosuppressive Circuits in the Crosstalk between Synovial Fibroblasts and Lymphocytes. Biomedicines. 2021, 9(10): 1413. 3. Luschnig P, Kienzl M, Roula D, et al. The JAK1/2 inhibitor baricitinib suppresses eosinophil effector function and restricts allergen-induced airway eosinophilia. Biochemical Pharmacology. 2021: 114690. 4. Kvacskay P, Yao N, Schnotz J H, et al. Increase of aerobic glycolysis mediated by activated T helper cells drives synovial fibroblasts towards an inflammatory phenotype: new targets for therapy. Arthritis Research & Therapy. 2021 Feb 15;23(1):56. doi: 10.1186/s13075-021-02437-7. 5. Kvacskay P, Yao N, Schnotz J H, et al. Increase of aerobic glycolysis mediated by activated T helper cells drives synovial fibroblasts towards an inflammatory phenotype: new targets for therapy?. Arthritis Research & Therapy. 2021, 23(1): 1-15.