Baricitinib (INCB028050)

For research use only.

Catalog No.S2851 Synonyms: LY3009104

23 publications

Baricitinib (INCB028050) Chemical Structure

CAS No. 1187594-09-7

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. Baricitinib is found to reduce or interrupt the passage of the virus into target cells and is used in the treatment research for COVID-19. Phase 3.

Selleck's Baricitinib (INCB028050) has been cited by 23 publications

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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. Baricitinib is found to reduce or interrupt the passage of the virus into target cells and is used in the treatment research for COVID-19. Phase 3.
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 NYrHb4dYTnWwY4Tpc44h[XO|YYm= NWjuV29uPDVibXnudy=> M3rrfGlvcGmkaYTpc44hd2ZiSlHLNkBpd22xZHnt[ZIhcW5iaIXtZY4hS0R|NDugZ4VtdHNic4Dpb4VlKGmwdH:gbJVu[W5id3jvcIUh[myxb3SgZZN{\XO|ZXSgZZMhcW6qaXLpeIlwdiCxZjDFVG8ucW6mdXPl[EBUXEGWLUWgdIhwe3Cqb4L5cIF1cW:wIIDy[Ylv[3WkYYTl[EBnd3JiNEWgcYlveyCob3zsc5dm\CCkeTDFVG8h[WSmaYTpc44hdWWjc4Xy[YQh[W[2ZYKgNVUhdWmwczDifUBHSUOVIHHuZYx6e2m|LDDJR|UxRTBwMEi3PO69VQ>? MnfDQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjR2MUe1N|MoRjJ2NEG3OVM{RC:jPh?=
human UT7 cells MnTGSpVv[3Srb36gZZN{[Xl? MY\Jcohq[mm2aX;uJI9nKEqDS{KgbY4hcHWvYX6gWXQ4KGOnbHzzJIF{e2W|c3XkJIF{KHO3cIDy[ZN{cW:wIH;mJGVRVy2|dHnteYxifGWmIGPURXQ2KHCqb4PwbI9zgWyjdHnvckBjgSCDbIDoZXNkemWnbjDhd5NigQ>? MnTpQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjZ|N{K2OVMoRjJ4M{eyOlU{RC:jPh?=
human TF1 cells M1qwOGZ2dmO2aX;uJIF{e2G7 NX32e4tFUW6qaXLpeIlwdiCxZjDKRWsyKGmwIHj1cYFvKFSIMTDj[YxteyCjc4Pld5Nm\CCjczDzeZBxemW|c3nvckBw\iCLTE[td5RqdXWuYYTl[EBUXEGWMzDwbI9{eGixconsZZRqd25iYomgRYxxcGGVY4Ll[Y4h[XO|YYm= MVi8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zPjN5Mk[1N{c,OjZ|N{K2OVM9N2F-
CD34+ MWLGeY5kfGmxbjDhd5NigQ>? NVy1fI52PDVibXnudy=> NVTFVJNFUW6qaXLpeIlwdiCxZjDKRWszKGixbX;kbY1meiCrbjDoeY1idiCFREO0L{Bk\WyuczDzdIls\WRiaX70c{BpfW2jbjD3bI9t\SCkbH;v[EBie3Onc4Pl[EBieyCrbnjpZol1cW:wIH;mJGVRVy2rbnT1Z4VlKFOWQWStOUBxcG:|cHjvdplt[XSrb36gdJJmcW6ldXLheIVlKG[xcjC0OUBucW6|IH\vcIxwf2WmIHL5JGVRVyCjZHTpeIlwdiCvZXHzeZJm\CCjZoTldkAyPSCvaX7zJIJ6KE[DQ2OgZY5idHm|aYOsJGlEPTBiPTCwMlA5PzhizszNMi=> MXS8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zPDRzN{WzN{c,OjR2MUe1N|M9N2F-
TF1 M2DQeWZ2dmO2aX;uJIF{e2G7 NVXlTXlKUW6qaXLpeIlwdiCxZjDKRWsyKGmwIHj1cYFvKFSIMTDj[YxteyCjc4Pld5Nm\CCjczDzeZBxemW|c3nvckBw\iCLTE[td5RqdXWuYYTl[EBUXEGWMzDwbI9{eGixconsZZRqd25iYomgRYxxcGGVY4Ll[Y4h[XO|YYmsJGlPUCB;IECuNFE4KM7:TT6= NHnuUXk9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{NkO3NlY2Oyd-Mk[zO|I3PTN:L3G+
UT7 MVPGeY5kfGmxbjDhd5NigQ>? NU\ZbFJVUW6qaXLpeIlwdiCxZjDKRWszKGmwIHj1cYFvKFWWNzDj[YxteyCjc4Pld5Nm\CCjczDzeZBxemW|c3nvckBw\iCHUF:td5RqdXWuYYTl[EBUXEGWNTDwbI9{eGixconsZZRqd25iYomgRYxxcGGVY4Ll[Y4h[XO|YYmsJGlPUCB;IECuN|Eh|ryPLh?= MVi8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zPjN5Mk[1N{c,OjZ|N{K2OVM9N2F-
HeLa NVX0OmEyTnWwY4Tpc44h[XO|YYm= M4fjR|UhfU1? NFTRS48zKGi{cx?= NGfBT|NKdmirYnn0bY9vKG:oIFnGUodidW2jLXnu[JVk\WRiSlHLNkBxcG:|cHjvdplt[XSrb36gbY4hcHWvYX6gTIVN[SClZXzsd{BifCB3IIXNJIlv[3WkYYTl[EBnd3JiMjDodpMh[nliV3XzeIVzdiCkbH;0JI1mfGixZB?= NYjKRo1IRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkexN|c{PTlpPkK3NVM4OzV7PD;hQi=>
A673 MVLxTHRUKGG|c3H5 NYHKd5J4eUiWUzDv[kBx\WSrYYTybYMh[2GwY3XyJINmdGxibHnu[ZMhfG9iaXTlcpRq\nlibYXseIlxdGVib4Dwc5J1fW6rdHnld{Bnd3JiZIL1[{Bz\XC3coDvd4lv\zpiUILpcYFzgSC|Y4Ll[Y4h\m:{IFG2O|Mh[2WubIO= MVu8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zQTR|NUGzPUc,Ojl2M{WxN|k9N2F-
SK-N-SH M131fZFJXFNiYYPzZZk> MkK0dWhVWyCxZjDw[YRq[XS{aXOgZ4Fv[2W{IHPlcIwhdGmwZYOgeI8hcWSnboTp[pkhdXWudHnwcIUhd3Cyb4L0eY5qfGmnczDmc5Ih\HK3ZzDy[ZB2enCxc3nu[|ohWHKrbXHyfUB{[3KnZX6g[o9zKFONLV6tV2gh[2WubIO= NIDySmE9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{OUSzOVE{QSd-Mkm0N|UyOzl:L3G+
NB1643 MmjUdWhVWyCjc4PhfS=> M1TDV5FJXFNib3[gdIVlcWG2cnnjJINidmOncjDj[YxtKGyrbnXzJJRwKGmmZX70bYZ6KG23bITpdIxmKG:ycH;yeJVvcXSrZYOg[o9zKGS{dXegdoVxfXKyb4Ppcoc7KFC{aX3hdpkhe2O{ZXXuJIZweiCQQkG2OFMh[2WubIO= M1zsfFxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ7NEO1NVM6Lz5{OUSzOVE{QTxxYU6=
Rh41 MnjCdWhVWyCjc4PhfS=> MkjidWhVWyCxZjDw[YRq[XS{aXOgZ4Fv[2W{IHPlcIwhdGmwZYOgeI8hcWSnboTp[pkhdXWudHnwcIUhd3Cyb4L0eY5qfGmnczDmc5Ih\HK3ZzDy[ZB2enCxc3nu[|ohWHKrbXHyfUB{[3KnZX6g[o9zKFKqNEGgZ4VtdHN? NHjJfYE9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{OUSzOVE{QSd-Mkm0N|UyOzl:L3G+
LAN-5 M17uSpFJXFNiYYPzZZk> M172TJFJXFNib3[gdIVlcWG2cnnjJINidmOncjDj[YxtKGyrbnXzJJRwKGmmZX70bYZ6KG23bITpdIxmKG:ycH;yeJVvcXSrZYOg[o9zKGS{dXegdoVxfXKyb4Ppcoc7KFC{aX3hdpkhe2O{ZXXuJIZweiCOQV6tOUBk\Wyucx?= NV7JdY52RGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkm0N|UyOzlpPkK5OFM2OTN7PD;hQi=>

... Click to View More Cell Line Experimental Data

Methods Test Index PMID
Western blot
phSTAT1 / phSTAT3 ; 

PubMed: 28369741     

Effect of Janus kinase (JAK) inhibition on phosphorylated signal transducer and activator of transcription (STAT) phosphorylation in RA neutrophils. Freshly isolated (0 h) RA neutrophils exhibited elevated levels of STAT-1 and STAT-3, which decreased during 60 min incubation in untreated conditions. Addition of baricitinib and tofacitinib (200 ng/ml) at 0 h induced a loss of phosphorylated STAT-1 and STAT-3 compared to untreated cells at 30 and 60 min.

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]


Animal Research:[1]
- Collapse
  • Animal Models: Collagen-induced arthritis (CIA) mice
  • 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 to the product individually and in order(Data is from Selleck tests instead of citations):
2% DMSO+30% PEG 300+5% Tween 80+ddH2O
For best results, use promptly after mixing.

* 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


CAS No. 1187594-09-7
Storage powder
in solvent
Synonyms LY3009104
Smiles CCS(=O)(=O)N1CC(C1)(CC#N)N2C=C(C=N2)C3=C4C=CNC4=NC=N3

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Clinical Trial Information

NCT Number Recruitment interventions Conditions Sponsor/Collaborators Start Date Phases
NCT04208464 Not yet recruiting Drug: Baricitinib Idiopathic Inflammatory Myopathies University of Manchester|Eli Lilly and Company|Manchester Clinical Trials Unit|Karolinska Institutet July 1 2020 Phase 2
NCT04358614 Completed Drug: Baricitinib 4 MG Oral Tablet COVID|Pneumonia Fabrizio Cantini|Hospital of Prato March 16 2020 Phase 2|Phase 3
NCT04088396 Recruiting Drug: Baricitinib|Drug: Placebo Systemic Juvenile Idiopathic Arthritis Eli Lilly and Company February 12 2020 Phase 3
NCT03952559 Recruiting Drug: Baricitinib|Drug: Placebo|Drug: Topical corticosteroid Atopic Dermatitis Eli Lilly and Company|Incyte Corporation May 24 2019 Phase 3
NCT03773978 Active not recruiting Drug: Baricitinib|Drug: Placebo Juvenile Idiopathic Arthritis Eli Lilly and Company December 17 2018 Phase 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