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Baricitinib (LY3009104, INCB028050) (Synonyms: INCB 028050, LY3009104)

Catalog No.GC14844

A JAK1 and JAK2 inhibitor

Products are for research use only. Not for human use. We do not sell to patients.

Baricitinib (LY3009104, INCB028050) Chemical Structure

Cas No.: 1187594-09-7

Taille Prix Stock Qté
10mM (in 1mL DMSO)
69,00 $US
En stock
1g
605,00 $US
En stock
500mg
378,00 $US
En stock
5mg
84,00 $US
En stock
10mg
112,00 $US
En stock
50mg
364,00 $US
En stock
100mg
595,00 $US
En stock
2mg
42,00 $US
En stock

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Sample solution is provided at 25 µL, 10mM.

Product Documents

Quality Control & SDS

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Protocol

Kinase experiment [1]:

Inhibitory activities

Enzyme assays were 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 fulllength enzyme (cMET and Chk2) and peptide substrate. Each enzyme reaction was performed with or without Baricitinib (LY3009104, INCB028050) (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 Baricitinib (LY3009104, INCB028050) concentration required for inhibition of 50% of the fluorescent signal. Additional kinase assays were 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, IKKa, IKKb, JNK1, Lck, MEK1, p38a, p70S6K, PKA, PKCa, Src, and ZAP70.

Cell experiment [1]:

Cell lines

Human PBMCs; PHA-stimulated T cells.

Preparation method

Soluble in DMSO > 10 mM. General tips for obtaining a higher concentration: Please warm the tube at 37℃ for 10 minutes and/or shake it in the ultrasonic bath for a while. Stock solution can be stored below -20℃ for several months.

Reaction Conditions

10, 100, 1000, 10000 nM; 48 h.

Applications

In PBMCs, INCB028050 inhibits STAT3 phosphorylation stimulated by IL-6 and the production of chemokine MCP-1 with IC50 values of 44 and 40 nM, respectively. In isolated naive T-cells, INCB028050 inhibits STAT3 phosphorylation with IC50 value of 20 nM and inhibits the production of IL-17 and IL-22 with IC50 value of 50 nM.

Animal experiment [1]:

Animal models

Female rats; adjuvant-induced arthritis rats; DBA/1j arthritis mice induced by bovine type II collagen.

Dosage form

Female rats: 10 mg/kg; 24 h; oral gavage.Adjuvant-induced arthritis rats: 1, 3, or 10 mg/kg; once daily for 2 wk; administrated orally.Collagen-induced arthritis (CIA) model: 1, 3, or 10 mg/kg; twice daily for 15 d; administrated orally.

Preparation method

Suspended in 0.5% methylcellulose and given by oral gavage at 10 ml/kg.

Applications

In female rats, INCB028050 (10 mg/kg) inhibits JAK1/2 signaling by ≥50% for 8 h. In rat adjuvant-induced arthritis, INCB028050 (1, 3, or 10 mg/kg) reduces disease scores by 24%, 57% and 81% respectively and inhibits the increase of hind paw volumes by 50%, >95% and >95%, respectively. Also, INCB028050 reduced bone resorption. In CIA mice model, INCB028050 (1, 3, or 10 mg/kg) reduces clinical scores by 19%, 67% and 61% respectively and inhibits IL-6 and IL-23 signaling and function.

Other notes

Please test the solubility of all compounds indoor, and the actual solubility may slightly differ with the theoretical value. This is caused by an experimental system error and it is normal.

References:

[1]. Fridman JS, Scherle PA, Collins R, et al. Selective inhibition of JAK1 and JAK2 is efficacious in rodent models of arthritis: preclinical characterization of INCB028050. J Immunol, 2010, 184(9): 5298-5307.

Background

Baricitinib, formerly named LY3009104 or INCB028050, is a new selective orally bioavailable inhibitor of tyrosine-protein kinase JAK1 or JAK2. Also, it is an ATP competitive kinase inhibitor. In vitro, it is able to inhibit JAK1 and JAK2 in a low nanomolar range with IC50 values of 5.9 and 5.7 nM, respectively, while it demonstrates low inhibitory activity for JAK3 and moderate activity for TYK2. Baricitinib inhibits intracellular signaling of multiple proinflammatory cytokines including IL-6 and IL-23 at concentrations <50 nM. It should also be recognized that JAK signaling is central to a number of fundamental processes, including the generation of RBCs

Reference

Gras, J. Baricitinib. Tyrosine-protein kinase JAK1/JAK2 inhibitor, treatment of rheumatoid arthritis. Drugs of the future. 2013, 38(9): 611.

Jordan S. Fridman, Peggy A. Scherle, Robert Collins, Timothy C. Burn, Yanlong Li, Jun Li, Maryanne B. Covington, Beth Thomas, Paul Collier, Margaret F. Favata, Xiaoming Wen, Jack Shi, Ryan McGee, Patrick J. Haley, Stacey Shepard, James D. Rodgers, Swamy Yeleswaram, Greg Hollis, Robert C. Newton, Brian Metcalf, Steven M. Friedman and Kris Vaddi. Selective Inhibition of JAK1 and JAK2 Is Efficacious in Rodent Models of Arthritis: Preclinical Characterization of INCB028050. The Journal of Immunology May 1, 2010 vol. 184 no. 9 5298-5307.

Chemical Properties

Cas No. 1187594-09-7 SDF
Synonymes INCB 028050, LY3009104
Chemical Name 2-[1-ethylsulfonyl-3-[4-(7H-pyrrolo[2,3-d]pyrimidin-4-yl)pyrazol-1-yl]azetidin-3-yl]acetonitrile
Canonical SMILES CCS(=O)(=O)N1CC(C1)(CC#N)N2C=C(C=N2)C3=C4C=CNC4=NC=N3
Formula C16H17N7O2S M.Wt 371.42
Solubility ≥ 18.57 mg/mL in DMSO Storage Store at -20°C
General tips Please select the appropriate solvent to prepare the stock solution according to the solubility of the product in different solvents; once the solution is prepared, please store it in separate packages to avoid product failure caused by repeated freezing and thawing.Storage method and period of the stock solution: When stored at -80°C, please use it within 6 months; when stored at -20°C, please use it within 1 month.
To increase solubility, heat the tube to 37°C and then oscillate in an ultrasonic bath for some time.
Shipping Condition Evaluation sample solution: shipped with blue ice. All other sizes available: with RT, or with Blue Ice upon request.

Complete Stock Solution Preparation Table

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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
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Average Rating: 5 ★★★★★ (Based on Reviews and 30 reference(s) in Google Scholar.)

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