[CAS NO. 1187594-09-7] Baricitinib (INCB028050)

Name: Baricitinib (INCB028050)
Brand: Arctom Scientific
SKU: SLK-S2851

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PRODUCTS SPECIFICATIONS [1187594-09-7]

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Catalog

SLK-S2851

Brand

Selleck

CAS

1187594-09-7

DESCRIPTION [1187594-09-7]

Overview

MDL	MFCD27920779
Molecular Weight	371.42
Molecular Formula	C16H17N7O2S
SMILES	C(C#N)C1(CN(S(CC)(=O)=O)C1)N2C=C(C=N2)C3=C4C(=NC=N3)NC=C4

For research use only.

Storage

3 years,-20°C,powder
1 years,-80°C,in solvent

Shipping

Room temperature shipping(Stability testing shows this product can be shipped without any cooling measures.)

Preparing Stock Solutions

Concentration Volume Mass	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
50 mM	0.0538 mL	0.2692 mL	0.5385 mL

Description

Baricitinib (LY3009104, INCB028050) is a selective and inhibitor with 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.

References

[1] Fridman JS, et al. J Immunol, 2010, 184(9), 5298-5307.
[2] Kontzias A, et al. Curr Opin Pharmacol, 2012, 12(4), 464-470.
[3] Norman P, et al. Expert Opin Ther Pat, 2012, 22(10), 1233-1249.
[4] Norman P, et al. Expert Opin Ther Pat, 2012, 22(9), 1105-1109.

Synonyms

3-Azetidineacetonitrile, 1-(ethylsulfonyl)-3-[4-(7H-pyrrolo[2,3-d]pyrimidin-4-yl)-1H-pyrazol-1-yl]-

1-(Ethylsulfonyl)-3-[4-(7H-pyrrolo[2,3-d]pyrimidin-4-yl)-1H-pyrazol-1-yl]-3-azetidineacetonitrile

LY 3009104

Baricitinib

INCB 028050

INCB 28050

Olumiant

2-(3-(4-(3H-Pyrrolo[2,3-d]pyrimidin-4-yl)-1H-pyrazol-1-yl)-1-(ethylsulfonyl)azetidin-3-yl)acetonitrile