Baricitinib (LY3009104, INCB028050)

Catalog No.S2851

Baricitinib (LY3009104, INCB028050) Chemical Structure

Molecular Weight(MW): 371.42

Baricitinib (LY3009104, INCB028050) is a selective JAK1 and JAK2 inhibitor with IC50 of 5.9 nM and 5.7 nM in cell-free assays, ~70 and ~10-fold selective versus JAK3 and Tyk2, no inhibition to c-Met and Chk2. Phase 3.

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2 Customer Reviews

  • bDNA analysis showing that the JAK1/2 inhibitors CYT387, AZD1480 and Baricitinib positively regulate UCP1 expression in PSC-WA. Values are mean ± s.d. of n = three biological replicates and differences from DMSO are significant for * P < 0.005. P values were calculated using the two-tailed paired Student's t-test.

    Nat Cell Biol,2014, 17(1):57-67. Baricitinib (LY3009104, INCB028050) purchased from Selleck.

    (A-C) Anti-proliferative activity of NDI-031301 (A), tofacitinib (B) or baricitinib (C) on transformed Ba/F3 cells. Ba/F3 cells transformed by TEL-ABL, TEL-JAK1, TEL-JAK2, TEL-JAK3, or TEL-TYK2 were cultured with graded concentrations of the indicated inhibitor for 72 h. Cell viability values are mean SD percentages of the untreated control value in triplicate experiments.

    Br J Haematol, 2017, 177(2):271-282. Baricitinib (LY3009104, INCB028050) purchased from Selleck.

Purity & Quality Control

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Biological Activity

Description Baricitinib (LY3009104, INCB028050) is a selective JAK1 and JAK2 inhibitor with IC50 of 5.9 nM and 5.7 nM in cell-free assays, ~70 and ~10-fold selective versus JAK3 and Tyk2, no inhibition to c-Met and Chk2. Phase 3.
Targets
JAK2 [1]
(Cell-free assay)
JAK1 [1]
(Cell-free assay)
TYK2 [1]
(Cell-free assay)
JAK3 [1]
(Cell-free assay)
5.7 nM 5.9 nM 53 nM >400 nM
In vitro

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 PBMCs. Baricitinib also inhibits pSTAT3 stimulated by IL-23 with IC50 od 20 nM in isolated naive T-cells. [1]

Cell Data
Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID
human CD34+ cells NIfhUpJHfW6ldHnvckBie3OjeR?= MnfkOFUhdWmwcx?= NX30OlRxUW6qaXLpeIlwdiCxZjDKRWszKGixbX;kbY1meiCrbjDoeY1idiCFREO0L{Bk\WyuczDzdIls\WRiaX70c{BpfW2jbjD3bI9t\SCkbH;v[EBie3Onc4Pl[EBieyCrbnjpZol1cW:wIH;mJGVRVy2rbnT1Z4VlKFOWQWStOUBxcG:|cHjvdplt[XSrb36gdJJmcW6ldXLheIVlKG[xcjC0OUBucW6|IH\vcIxwf2WmIHL5JGVRVyCjZHTpeIlwdiCvZXHzeZJm\CCjZoTldkAyPSCvaX7zJIJ6KE[DQ2OgZY5idHm|aYOsJGlEPTB;MD6wPFc5|ryP NGrvdm8zPDRzN{WzNy=>
human UT7 cells MWfGeY5kfGmxbjDhd5NigQ>? NFHxcmFKdmirYnn0bY9vKG:oIFrBT|IhcW5iaIXtZY4hXVR5IHPlcIx{KGG|c3Xzd4VlKGG|IIP1dJBz\XO|aX;uJI9nKEWSTz3zeIlufWyjdHXkJHNVSVR3IIDoc5NxcG:{eXzheIlwdiCkeTDBcJBp[VOlcnXlckBie3OjeR?= NFvx[mQzPjN5Mk[1Ny=>
human TF1 cells MonPSpVv[3Srb36gZZN{[Xl? NXXY[XllUW6qaXLpeIlwdiCxZjDKRWsyKGmwIHj1cYFvKFSIMTDj[YxteyCjc4Pld5Nm\CCjczDzeZBxemW|c3nvckBw\iCLTE[td5RqdXWuYYTl[EBUXEGWMzDwbI9{eGixconsZZRqd25iYomgRYxxcGGVY4Ll[Y4h[XO|YYm= NHP5[GszPjN5Mk[1Ny=>

... Click to View More Cell Line Experimental Data

In vivo Baricitinib inhibits IL-6–stimulated phosphorylation of STAT3 in whole blood with an IC50 of 128 nM. Baricitinib (10 mg/kg p.o.) is expected to inhibit JAK1/2 signaling (by ≥50%) in rats for about 8 hours. Baricitinib (10 mg/mL, p.o.) inhibits disease scores in dose-dependent manner in rats with established disease in the adjuvant arthritis model. Baricitinib treatment, compared with vehicle, inhibits the increase in hind paw volumes during the 2 weeks of treatment by 50% at a dose of 1 mg/kg and >95% at doses of 3 mg/kg or 10 mg/kg. Baricitinib treatment, compared with vehicle, also inhibits composite score of immune infiltrate, edema, and periarticular tissue appearance by 27% at a dose of 1 mg/kg, 64% at doses of 3 mg/kg and 82% at doses of 10 mg/kg in rats with established disease in the adjuvant arthritis model. Baricitinib reduces bone resorption by 15%, 61%, and 67% with increasing dose level (1, 3, and 10 mg/kg) in rats with established disease in the adjuvant arthritis model. Baricitinib (10 mg/kg, daily for 2 wk, p.o.) results in radiographic improvements with restoration of the normal architecture and appearance to the ankle and tarsals in rats with established disease in the adjuvant arthritis model. Baricitinib reduces levels of pSTAT3 in a dose- and time-dependent manner in the peripheral blood of rAIA animals. Baricitinib (10 mg/mL, p.o.) improves a composite score of joint damage by 47% in the murine CIA model. Baricitinib (10 mg/kg) reduces pannus (74%) and bone damage (78%) and improves cartilage damage (43%) and signs of inflammation (33%), resulting in a 53% improvement in an aggregate score of disease in the collagen Ab-induced arthritis (CAIA) murine model. Baricitinib (10 mg/kg) inhibits the delayed-type hypersensitivity response by 48% in both the CIA and CAIA models. [1] Baricitinib is efficacious in active rheumatoid arthritis patients refractory to disease modifying drugs and biologics. [2] Baricitinib preferentially inhibits JAK1 and JAK2, with 10-fold selectivity over Tyk2 and 100-fold over JAK3. The observed effects of GLPG-0634 on the ACR20, albeit in a smaller study, appear to be at least as good as that seen with tofacitinib and superior to that of baricitinib, since baricitinib only moderately affect the ACR20 values in Phase IIa clinical studies. [3] Baricitinib has the dose-limiting side-effect of inducing anaemia which has been attributed to its effects on JAK2 but has clearly shown efficacy. [4]

Protocol

Animal Research:[1]
+ Expand
  • Animal Models: Collagen-induced arthritis (CIA) mice
  • Formulation: 0.5% methylcellulose
  • Dosages: 10 mg/mL
  • Administration: orally
    (Only for Reference)

Solubility (25°C)

In vitro DMSO 74 mg/mL (199.23 mM)
Water Insoluble
Ethanol Insoluble
In vivo Add solvents individually and in order:
2% DMSO+30% PEG 300+5% Tween 80+ddH2O
5mg/mL

* Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations.

Chemical Information

Molecular Weight 371.42
Formula

C16H17N7O2S

CAS No. 1187594-09-7
Storage powder
Synonyms N/A

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Clinical Trial Information

NCT Number Recruitment Conditions Sponsor/Collaborators Start Date Phases
NCT02759731 Recruiting Chronic Graft vs Host Disease|Chronic Graft-Versus-Host Disease National Cancer Institute (NCI)|National Institutes of Health Clinical Center (CC) April 8, 2016 Phase 1|Phase 2
NCT02758613 Completed Healthy Eli Lilly and Company May 2016 Phase 1
NCT02708095 Recruiting Systemic Lupus Erythematosus Eli Lilly and Company March 2016 Phase 2
NCT02576938 Active, not recruiting Atopic Dermatitis Eli Lilly and Company February 2016 Phase 2
NCT02340104 Completed Healthy Volunteers Eli Lilly and Company January 2015 Phase 1
NCT02263911 Completed Healthy Volunteers Eli Lilly and Company November 2014 Phase 1

Tech Support

Answers to questions you may have can be found in the inhibitor handling instructions. Topics include how to prepare stock solutions, how to store inhibitors, and issues that need special attention for cell-based assays and animal experiments.

Handling Instructions

Tel: +1-832-582-8158 Ext:3

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Frequently Asked Questions

  • Question 1:

    Do you know if S2851 will dissolve directly into 0.5% methylcellulose (vehicle for oral gavage treatments) or is acid required to dissolve it?

  • Answer:

    S2851 dissolve directly into 0.5% methylcellulose, and this is cited from the reference. We also test that dissolve S2851 into 30% PEG400/0.5% Tween80/5% propylene glycol. The solubility is about 30 mg/mL.

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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID