A JAK1 and JAK2 inhibitor
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Baricitinib

Item No. 16707

Technical Information
Formal Name
1-(ethylsulfonyl)-3-[4-(7H-pyrrolo[2,3-d]pyrimidin-4-yl)-1H-pyrazol-1-yl]-3-azetidineacetonitrile
CAS Number
1187594-09-7
Synonyms
  • INCB 028050
  • LY3009104
Molecular Formula
C16H17N7O2S
Formula Weight
Purity
≥95%
A crystalline solid
DMF: 50 mg/mlDMF:PBS(pH 7.2)(1:1): 0.5 mg/mlDMSO: 30 mg/ml
λmax
225, 250, 310 nm
SMILES
O=S(N(C1)CC1(CC#N)N(N=C2)C=C2C3=C4C(NC=C4)=NC=N3)(CC)=O
InChi Code
InChI=1S/C16H17N7O2S/c1-2-26(24,25)22-9-16(10-22,4-5-17)23-8-12(7-21-23)14-13-3-6-18-15(13)20-11-19-14/h3,6-8,11H,2,4,9-10H2,1H3,(H,18,19,20)
InChi Key
XUZMWHLSFXCVMG-UHFFFAOYSA-N
Shipping & Storage Information
Storage
-20°C
Shipping
Room temperature in continental US; may vary elsewhere
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    Product Description

    Baricitinib is an inhibitor of JAK1 and JAK2 (IC50s = 0.0059 and 0.0057 µM, respectively).1 It is selective for JAK1 and JAK2 over JAK3, TYK2, c-Met, and checkpoint kinase 2 (Chk2; IC50s = >0.4, 0.053, >10, and >1 µM, respectively). Baricitinib inhibits IL-6-induced phosphorylation of STAT3 in isolated human peripheral blood mononuclear cells (PBMCs) and rat whole blood (IC50s = 0.044 and 0.128 µM, respectively). It reduces disease severity in a type II collagen-induced mouse model of arthritis when administered at doses of 3 and 10 mg/kg. Baricitinib (4 mg/animal) also decreases lung macrophage infiltration and disease severity in rhesus monkeys infected with severe acute respiratory syndrome coronavirus 2 (SARS-CoV-2).2 Formulations containing baricitinib have been used in the treatment of rheumatoid arthritis.

    WARNING This product is not for human or veterinary use.

    References & Product Citations
    Product Description References

    1. Fridman, J.S., Scherle, P.A., Collins, R., et alSelective inhibition of JAK1 and JAK2 is efficacious in rodent models of arthritis: Preclinical characterization of INCB028050. J. Immunol. 184(9), 5298-5307 (2010).

    2. Hoang, T.N., Pino, M., Boddapati, A.K., et alBaricitinib treatment resolves lower-airway macrophage inflammation and neutrophil recruitment in SARS-CoV-2-infected rhesus macaques. Cell 184(2), 460-475 (2021).