Baricitinib

Catalog No.S2851 Batch:S285104

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Technical Data

Formula

C16H17N7O2S
Molecular Weight 371.42 CAS No. 1187594-09-7
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)
Clear solution
5%DMSO 40%PEG 300 5%Tween80 50% ddH2O
2.5mg/ml Taking the 1 mL working solution as an example, add 50 μL of 50 mg/mL clarified DMSO stock solution to 400 μL PEG300, mix evenly to clarify; add 50 μL Tween-80 to the above system, mix evenly to clarify; Then continue to add 500 μL ddH2O to adjust the volume to 1 mL. The mixed solution should be used immediately for optimal results. 
* <1 mg/ml means slightly soluble or insoluble.
* 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.
* Room temperature shipping (Stability testing shows this product can be shipped without any cooling measures.)

Preparing Stock Solutions

Biological Activity

Description Baricitinib 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.
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]
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 (from reference)

Kinase Assay:

[1]
  • Biochemical assays

    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.
Animal Study:

[1]
  • Animal Models

    Collagen-induced arthritis (CIA) mice

  • Dosages

    10 mg/mL

  • Administration

    orally

Customer Product Validation

, , Nat Cell Biol,2014, 17(1):57-67

Data from [Data independently produced by , , Br J Haematol, 2017, 177(2):271-282]

Data from [Data independently produced by , , J Physiol, 2015, 593(24):5269-82]

Data from [Data independently produced by , , Sci Rep, 2018, 8(1):15645]

Selleck's Baricitinib has been cited by 59 publications

Macrophage re-programming by JAK inhibitors relies on MAFB [ Cell Mol Life Sci, 2024, 81(1):152] PubMed: 38528207
A panel of janus kinase inhibitors identified with anti-inflammatory effects protect mice from lethal influenza virus infection [ Antimicrob Agents Chemother, 2024, 68(4):e0135023.] PubMed: 38470034
Pacritinib inhibits proliferation of primary effusion lymphoma cells and production of viral interleukin-6 induced cytokines [ Sci Rep, 2024, 14(1):4125] PubMed: 38374336
Novel JAK Inhibitors to Reduce Graft-Versus-Host Disease after Allogeneic Hematopoietic Cell Transplantation in a Preclinical Mouse Model [ Molecules, 2024, 29(8)1801] PubMed: 38675621
Activation of endogenous retroviruses and induction of viral mimicry by MEK1/2 inhibition in pancreatic cancer [ Sci Adv, 2024, 10(13):eadk5386] PubMed: 38536927
Interferon signaling promotes tolerance to chromosomal instability during metastatic evolution in renal cancer [ Nat Cancer, 2023, 4(7):984-1000] PubMed: 37365326
Interferon signaling promotes tolerance to chromosomal instability during metastatic evolution in renal cancer [ Nat Cancer, 2023, 4(7):984-1000] PubMed: 37365326
Matrix mechanics regulate the polarization state of bone marrow-derived neutrophils through the JAK1/STAT3 signaling pathway [ Acta Biomater, 2023, 168:159-173] PubMed: 37467837
EndoC-βH5 cells are storable and ready-to-use human pancreatic beta cells with physiological insulin secretion [ Mol Metab, 2023, 76:101772] PubMed: 37442376
Effect of JAK inhibitors on the three forms of bone damage in autoimmune arthritis: joint erosion, periarticular osteopenia, and systemic bone loss [ Inflamm Regen, 2023, 43(1):44] PubMed: 37726797

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SHIPPING AND STORAGE
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