Baricitinib

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Cat.No. 7222 - Baricitinib | C16H17N7O2S | CAS No. 1187594-09-7
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)
Datasheet
Citations
Reviews
Literature (3)
Pathways (1)

Biological Activity

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 (Kd 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.

Technical Data

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 Data

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

Preparing Stock Solutions

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.

Select a batch to recalculate based on the batch molecular weight:
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

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

Fridman et al (2010) Selective inhibition of JAK1 and JAK2 is efficacious in rodent models of arthritis: preclinical characterization of INCB028050. J.Immunol. 184 5298 PMID: 20363976

Sorrell et al (2016) Family-wide structural analysis of human numb-associated protein kinases. Structure. 24 401 PMID: 26853940

Richardson et al (2020) Baricitinib as potential treatment for 2019-nCoV acute respiratory disease. Lancet. 395 e30 PMID: 32032529


If you know of a relevant reference for Baricitinib, please let us know.

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Citations for Baricitinib

Citations are publications that use Tocris products.

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Literature in this Area

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Cancer

Cancer Research Product Guide

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Kinases Product Listing

A collection of over 400 products for kinase research, the listing includes inhibitors of:

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Pathways for Baricitinib

JAK-STAT

JAK-STAT Signaling Pathway

The JAK-STAT signaling pathway has several roles, including the control of cell proliferation and hematopoiesis. It is the main signal transduction cascade from cytokine receptors.