Baricitinib

Name: Baricitinib
Brand: Tocris Bioscience
SKU: 7222

Tocris Bioscience, part of Bio-Techne | Catalog # 7222

Citations (6)

COA / SDS

Highly potent JAK1 and JAK2 inhibitor; also inhibits JAK3 and Tyk2

Key Product Details

Description:	Highly potent JAK1 and JAK2 inhibitor; also inhibits JAK3 and Tyk2
Alternative Names:	INCB 28050
Chemical Name:	1-(Ethylsulfonyl)-3-[4-(7H-pyrrolo[2,3-d]pyrimidin-4-yl)-1H-pyrazol-1-yl]-3-azetidineacetonitrile
Purity:	≥98% (HPLC)
Molecular Weight:	371.42

View Full Technical Details for Baricitinib

Technical Data
Citations

Biological Activity for Baricitinib

Baricitinib is a highly potent JAK1 and JAK2 inhibitor (IC₅₀ values are 5.9 and 5.7 nM, respectively). Also inhibits Tyk2 (IC₅₀ = 53 nM). Displays >100-fold selectivity for JAK1/2 over JAK3 (IC₅₀ = 53 nM for JAK3). Binds AAK1, BIKE, GAK and MPSK1 in vitro (K_d values are 17.2, 39.8, 134.4 and 68.5 nM, respectively). Inhibits IL-6-induced STAT phosphorylation and subsequent pro-inflammatory chemokine (MPC-1) and cytokine (IL-17 and IL-22) production in PBMCs and T-cells. Displays anti-inflammatory and disease modifying effects in the rat adjuvant arthritis model. In silico modelling predicts inhibition of SARS-CoV-2 cell entry.

Compound Libraries for Baricitinib

Baricitinib is also offered as part of the Tocriscreen Kinase Inhibitor Library, Tocriscreen Antiviral Library and Tocriscreen Epigenetics Library. Find out more about compound libraries available from Tocris.

Technical Data for Baricitinib

M. Wt	371.42
Formula	C₁₆H₁₇N₇O₂S
Storage	Store at -20°C
Purity	≥98% (HPLC)
CAS Number	1187594-09-7
PubChem ID	44205240
InChi Key	XUZMWHLSFXCVMG-UHFFFAOYSA-N
Smiles	CCS(=O)(N1CC(C1)(N2C=C(C3=C4C=CNC4=NC=N3)C=N2)CC#N)=O

The technical data provided above is for guidance only. For batch specific data refer to the Certificate of Analysis.

Tocris products are intended for laboratory research use only, unless stated otherwise.

Solubility for Baricitinib

	Solvent	Max Conc. mg/mL	Max Conc. mM
Solubility
Solubility	DMSO	37.14	100

Preparing Stock Solutions for Baricitinib

The following data is based on the product molecular weight 371.42.

Batch specific molecular weights may vary from batch to batch due to the degree of hydration, which will affect the solvent volumes required to prepare stock solutions.

Concentration / Solvent Volume / Mass	1 mg	5 mg	10 mg
1 mM	2.69 mL	13.46 mL	26.92 mL
5 mM	0.54 mL	2.69 mL	5.38 mL
10 mM	0.27 mL	1.35 mL	2.69 mL
50 mM	0.05 mL	0.27 mL	0.54 mL

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References for Baricitinib

References are publications that support the biological activity of the product.

Sorrell Family-wide structural analysis of human numb-associated protein kinases. Structure. 2016 PMID: 26853940
Richardson Baricitinib as potential treatment for 2019-nCoV acute respiratory disease. Lancet. 2020 PMID: 32032529
Fridman Selective inhibition of JAK1 and JAK2 is efficacious in rodent models of arthritis: preclinical characterization of INCB028050. J.Immunol. 2010 PMID: 20363976