1. Epigenetics
    Stem Cell/Wnt
    JAK/STAT Signaling
  2. JAK

Baricitinib (Synonyms: INCB028050; LY3009104)

Cat. No.: HY-15315 Purity: 99.70%
Data Sheet SDS Handling Instructions

Baricitinib is a selective orally bioavailable JAK1/JAK2 inhibitor with IC50 of 5.9 nM and 5.7 nM, respectively.

For research use only. We do not sell to patients.
Baricitinib Chemical Structure

Baricitinib Chemical Structure

CAS No. : 1187594-09-7

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Other Forms of Baricitinib:

    Baricitinib purchased from MCE. Usage Cited in: PLoS One. 2017 Jul 14;12(7):e0181126.

    An activator of Stat3, colivelin (0.1 or 1 µM), rescued Baricitinib-induced RANKL down-regulation in osteoblast cultures.
    • Biological Activity

    • Protocol

    • Technical Information

    • Purity & Documentation

    • References

    Description

    Baricitinib is a selective orally bioavailable JAK1/JAK2 inhibitor with IC50 of 5.9 nM and 5.7 nM, respectively.

    IC50 & Target

    IC50: 5.9 nM (JAK1), 5.7 nM (JAK2), >400 (JAK3), 53 nM (Tyk2)[1]

    In Vitro

    In cell-based assays, Baricitinib (INCB028050) proves to be a potent inhibitor of JAK signaling and function. In PBMCs, Baricitinib inhibits IL-6-stimulated phosphorylation of the canonical substrate STAT3 (pSTAT3) and subsequent production of the chemokine MCP-1 with IC50 values of 44 nM and 40 nM, respectively. In isolated naive T-cells, INCB028050 also inhibits pSTAT3 stimulated by IL-23 (IC50=20 nM). Importantly, this inhibition prevented the production of two pathogenic cytokines (IL-17 and IL-22) produced by Th17 cells-a subtype of helper T cells with demonstrable inflammatory and pathogenic properties-with an IC50 value of 50 nM. In stark contrast, the structurally similar but ineffective JAK1/2 inhibitors INCB027753 and INCB029843 has no significant effect in any of these assays systems when tested at concentrations up to 10 μM[1].

    In Vivo

    Baricitinib (INCB028050) treatment, compares with vehicle, inhibits the increase in hind paw volumes during the 2 wk of treatment by 50% at a dose of 1 mg/kg and >95% at doses of 3 or 10 mg/kg. Because baseline paw volume measurements are taken on treatment day 0-in animals with significant signs of disease-it is possible to have >100% inhibition in animals showing marked improvement in swelling[1]. Baricitinib (0.7 mg/day) treated mice exhibits substantially reduced inflammation as assessed by H&E staining, reduced CD8 infiltration, and reduced MHC class I and class II expression when compared with vehicle-control treated mice. CD8+NKG2D+ cells, critical effectors of disease in murine and human alopecia areata (AA), are greatly diminished in Baricitinib treated mice compare with vehicle control treated mice[2].

    Clinical Trial
    NCT Number Sponsor Condition Start Date Phase
    NCT02340104 Eli Lilly and Company Healthy Volunteers January 2015 Phase 1
    NCT01870388 Eli Lilly and Company Liver Diseases|Hepatic Insufficiency June 2013 Phase 1
    NCT01968057 Eli Lilly and Company Healthy Volunteers October 2013 Phase 1
    NCT01925144 Eli Lilly and Company Healthy Volunteers October 2013 Phase 1
    NCT01910311 Eli Lilly and Company Healthy Volunteers August 2013 Phase 1
    NCT02263911 Eli Lilly and Company Healthy Participants November 2014 Phase 1
    NCT03026504 Matthew J Koster|Eli Lilly and Company|Mayo Clinic Arteritis, Giant Cell March 9, 2017 Phase 2
    NCT03212638 Eli Lilly and Company Healthy June 27, 2017 Phase 1
    NCT01490632 Eli Lilly and Company|Incyte Corporation Psoriasis|Skin Diseases|Skin Diseases, Papulosquamous December 2011 Phase 2
    NCT01859078 Eli Lilly and Company Healthy Volunteers May 2013 Phase 1
    NCT01896726 Eli Lilly and Company Healthy Volunteers July 2013 Phase 1
    NCT01937026 Eli Lilly and Company Healthy Volunteers September 2013 Phase 1
    NCT01924299 Eli Lilly and Company Healthy Volunteers August 2013 Phase 1
    NCT02708095 Eli Lilly and Company Systemic Lupus Erythematosus March 2016 Phase 2
    NCT02759731 National Cancer Institute (NCI)|National Institutes of Health Clinical Center (CC) Chronic Graft vs Host Disease|Chronic Graft-Versus-Host Disease April 8, 2016 Phase 1|Phase 2
    NCT02265705 Eli Lilly and Company Rheumatoid Arthritis October 2014 Phase 3
    NCT01960140 Eli Lilly and Company Healthy Volunteers October 2013 Phase 1
    NCT02576938 Eli Lilly and Company Atopic Dermatitis February 2016 Phase 2
    NCT01683409 Eli Lilly and Company|Incyte Corporation Diabetic Kidney Disease August 2012 Phase 2
    NCT01885078 Eli Lilly and Company Rheumatoid Arthritis June 2013 Phase 3
    NCT01721044 Eli Lilly and Company Rheumatoid Arthritis January 2013 Phase 3
    NCT01710358 Eli Lilly and Company Rheumatoid Arthritis October 2012 Phase 3
    NCT01721057 Eli Lilly and Company Rheumatoid Arthritis December 2012 Phase 3
    NCT01711359 Eli Lilly and Company Rheumatoid Arthritis November 2012 Phase 3
    NCT01724580 Eli Lilly and Company Chronic Atypical Neutrophilic Dermatosis With Lipodystrophy and Elevated Temperature (CANDLE)|Juvenile Dermatomyositis (JDM)|Stimulator of Interferon Genes (STING)-Associated Vasculopathy With Onset During Infancy (SAVI)|Aicardi-Goutières Syndrome (AGS)
    NCT02340104 Eli Lilly and Company Healthy Volunteers January 2015 Phase 1
    NCT01870388 Eli Lilly and Company Liver Diseases|Hepatic Insufficiency June 2013 Phase 1
    NCT01968057 Eli Lilly and Company Healthy Volunteers October 2013 Phase 1
    NCT01925144 Eli Lilly and Company Healthy Volunteers October 2013 Phase 1
    NCT01910311 Eli Lilly and Company Healthy Volunteers August 2013 Phase 1
    NCT02263911 Eli Lilly and Company Healthy Participants November 2014 Phase 1
    NCT03026504 Matthew J Koster|Eli Lilly and Company|Mayo Clinic Arteritis, Giant Cell March 9, 2017 Phase 2
    NCT03212638 Eli Lilly and Company Healthy June 27, 2017 Phase 1
    NCT01490632 Eli Lilly and Company|Incyte Corporation Psoriasis|Skin Diseases|Skin Diseases, Papulosquamous December 2011 Phase 2
    NCT01859078 Eli Lilly and Company Healthy Volunteers May 2013 Phase 1
    NCT01896726 Eli Lilly and Company Healthy Volunteers July 2013 Phase 1
    NCT01937026 Eli Lilly and Company Healthy Volunteers September 2013 Phase 1
    NCT01924299 Eli Lilly and Company Healthy Volunteers August 2013 Phase 1
    NCT02708095 Eli Lilly and Company Systemic Lupus Erythematosus March 2016 Phase 2
    NCT02759731 National Cancer Institute (NCI)|National Institutes of Health Clinical Center (CC) Chronic Graft vs Host Disease|Chronic Graft-Versus-Host Disease April 8, 2016 Phase 1|Phase 2
    NCT02265705 Eli Lilly and Company Rheumatoid Arthritis October 2014 Phase 3
    NCT01960140 Eli Lilly and Company Healthy Volunteers October 2013 Phase 1
    NCT02576938 Eli Lilly and Company Atopic Dermatitis February 2016 Phase 2
    NCT01683409 Eli Lilly and Company|Incyte Corporation Diabetic Kidney Disease August 2012 Phase 2
    NCT01885078 Eli Lilly and Company Rheumatoid Arthritis June 2013 Phase 3
    NCT01721044 Eli Lilly and Company Rheumatoid Arthritis January 2013 Phase 3
    NCT01710358 Eli Lilly and Company Rheumatoid Arthritis October 2012 Phase 3
    NCT01721057 Eli Lilly and Company Rheumatoid Arthritis December 2012 Phase 3
    NCT01711359 Eli Lilly and Company Rheumatoid Arthritis November 2012 Phase 3
    NCT01724580 Eli Lilly and Company Chronic Atypical Neutrophilic Dermatosis With Lipodystrophy and Elevated Temperature (CANDLE)|Juvenile Dermatomyositis (JDM)|Stimulator of Interferon Genes (STING)-Associated Vasculopathy With Onset During Infancy (SAVI)|Aicardi-Goutières Syndrome (AGS)
    NCT00902486 Incyte Corporation Rheumatoid Arthritis May 2009 Phase 2
    NCT01299285 Eli Lilly and Company Healthy Volunteers February 2011 Phase 1
    NCT01536951 Eli Lilly and Company|Incyte Corporation Healthy Participants February 2012 Phase 1
    NCT02758613 Eli Lilly and Company Healthy May 2016 Phase 1
    NCT01247350 Eli Lilly and Company Healthy Volunteer November 2010 Phase 1
    NCT01398475 Eli Lilly and Company|Incyte Corporation Chronic Inflammatory Disorder|Arthritis, Rheumatoid July 2011 Phase 1
    NCT01185353 Eli Lilly and Company|Incyte Corporation Arthritis, Rheumatoid October 2010 Phase 2
    NCT01469013 Eli Lilly and Company Arthritis, Rheumatoid November 2011 Phase 2
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    References
    Preparing Stock Solutions
    Concentration Volume (DMSO) Mass 1 mg 5 mg 10 mg
    1 mM 2.6924 mL 13.4618 mL 26.9237 mL
    5 mM 0.5385 mL 2.6924 mL 5.3847 mL
    10 mM 0.2692 mL 1.3462 mL 2.6924 mL
    Kinase Assay
    [1]

    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]. MCE has not independently confirmed the accuracy of these methods. They are for reference only.

    Cell Assay
    [1]

    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]. MCE has not independently confirmed the accuracy of these methods. They are for reference only.

    Animal Administration
    [1][2]

    Baricitinib (INCB 028050) is suspended in 0.5% methylcellulose (Rat)[1].

    Rat[1]
    Female rats (n=6 per gender per group) are given a dose of 10 mg/kg Baricitinib and given by oral gavage at 10 mL/kg. The first three rats are bled at 0 (predose), 2, 8, and 24 h, and the second three rats are bled 1, 4, and 12 h after dosing. EDTA is used as the anticoagulant, and samples are centrifuged to obtain plasma. An analytical method for the quantification of INCB028050 has been developed and used to analyze samples from toxicology studies. The method combines a protein precipitation extraction with 10% methanol in acetonitrile and LC/MS/MS analysis. The method has demonstrated a linear assay range 1-5000 nM using 0.1 mL of study samples. Data are processed using Analyst 1.3.1. A standard curve is determined from peak area ratio versus concentration using a weighted linear regression (1/x2).
    Mice[2]
    The C3H/HeJ graft-recipient mouse model of AA is used for these experiments. Briefly, alopecic skin from a C3H/HeJ mouse that spontaneously developed hair loss is grafted onto 8-10 week old C3H/HeJ mice free of disease. At the time of grafting, an osmotic pump that administered approximately 0.7 mg/day of Baricitinib or placebo is implanted. Osmotic pumps are changed monthly. A time-to-event survival analysis for interval censored data is performed. The survival and interval packages in R are used to perform log-rank tests. The hypothesis that the survival distributions are equal in the (n=10) Baricitinib-treated mice and (n=10) placebo-treated mice is rejected at the 5% level using Sun's score to perform an exact log-rank two-sample test with the p-value of 0.0035. MCE has not independently confirmed the accuracy of these methods. They are for reference only.

    References
    Molecular Weight

    371.42

    Formula

    C₁₆H₁₇N₇O₂S

    CAS No.

    1187594-09-7

    Storage

    Please store the product under the recommended conditions in the Certificate of Analysis.

    Shipping

    Room temperature in continental US; may vary elsewhere

    Solvent & Solubility

    DMSO: 25 mg/mL

    Baricitinib is suspended in 0.5% methylcellulose[3].

    * "<1 mg/mL" means slightly soluble or insoluble. "≥" means soluble, but saturation unknown.

    References

    Purity: 99.70%

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    Baricitinib
    Cat. No.:
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