CAS 575474-82-7|R 112

Introduction：Basic information about CAS 575474-82-7|R 112, including its chemical name, molecular formula, synonyms, physicochemical properties, and safety information, etc.

Table of Contents

1. Names
2. R 112 BiologicalActivity
3. Chemical & Physical Properties
4. Synonyms

Common Name	R 112
CAS Number	575474-82-7	Molecular Weight	312.29800
Density	/	Boiling Point	/
Molecular Formula	C₁₆H₁₃FN₄O₂	Melting Point	/
MSDS	/	Flash Point	/

Names

Name	3,3'-[(5-Fluoro-2,4-pyrimidinediyl)diimino]diphenol
Synonym	More Synonyms

R 112 BiologicalActivity

Description	R112 is an ATP-competitive inhibitor of Syk kinase with a Ki of 96 nM. R112 inhibits Syk kinase activity with an IC50 of 226 nM. IC50 value: 226 nM [1]Target: Sykin vitro: R112 blocks leukotriene C4 production and all proinflammatory cytokines tested. Its onset of action was immediate, and the inhibition was reversible. R112 is able to completely inhibit all three IgE-induced mast cell functions: degranulation, lipid mediator production, and cytokine production. R112 potently, completely, and rapidly abrogated all mast cell activation cascades triggered by IgE receptor cross-linking.[1]
Related Catalog	Signaling Pathways >>Protein Tyrosine Kinase/RTK >>SykResearch Areas >>Inflammation/Immunology
References	[1]. Rossi AB, et al. Identification of the Syk kinase inhibitor R112 by a human mast cell screen. J Allergy Clin Immunol. 2006 Sep;118(3):749-755. [2]. Meltzer EO, et al. An intranasal Syk-kinase inhibitor (R112) improves the symptoms of seasonal allergic rhinitis in a park environment. J Allergy Clin Immunol. 2005 Apr;115(4):791-796.

Description

R112 is an ATP-competitive inhibitor of Syk kinase with a Ki of 96 nM. R112 inhibits Syk kinase activity with an IC50 of 226 nM. IC50 value: 226 nM [1]Target: Sykin vitro: R112 blocks leukotriene C4 production and all proinflammatory cytokines tested. Its onset of action was immediate, and the inhibition was reversible. R112 is able to completely inhibit all three IgE-induced mast cell functions: degranulation, lipid mediator production, and cytokine production. R112 potently, completely, and rapidly abrogated all mast cell activation cascades triggered by IgE receptor cross-linking.[1]

Related Catalog

Signaling Pathways >>Protein Tyrosine Kinase/RTK >>SykResearch Areas >>Inflammation/Immunology

References

[1]. Rossi AB, et al. Identification of the Syk kinase inhibitor R112 by a human mast cell screen. J Allergy Clin Immunol. 2006 Sep;118(3):749-755.

[2]. Meltzer EO, et al. An intranasal Syk-kinase inhibitor (R112) improves the symptoms of seasonal allergic rhinitis in a park environment. J Allergy Clin Immunol. 2005 Apr;115(4):791-796.

Chemical & Physical Properties

Molecular Formula	C₁₆H₁₃FN₄O₂
Molecular Weight	312.29800
Exact Mass	312.10200
PSA	93.53000
LogP	3.00900
Appearance of Characters	offwhite solid
InChIKey	TVKGTSHBQZEFEE-UHFFFAOYSA-N
SMILES	Oc1cccc(Nc2ncc(F)c(Nc3cccc(O)c3)n2)c1

Synonyms

R 112

R112

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