Home Angiogenesis Syk inhibitor R112 For research use only.

R112

R112 is an ATP-competitive spleen tyrosine kinase (Syk) inhibitor with Ki value of 96 nM.

R112 Chemical Structure

R112 Chemical Structure

CAS: 575474-82-7

Purity & Quality Control

Batch: S651901 DMSO] 62 mg/mL] false] Water] Insoluble] false] Ethanol] Insoluble] false Purity: 99.56%
99.56

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Biological Activity

Description R112 is an ATP-competitive spleen tyrosine kinase (Syk) inhibitor with Ki value of 96 nM.
Targets
Syk [1]
(Cell-free assay)
96 nM(Ki)
In vitro
In vitro

R112 inhibits degranulation induced by anti-IgE cross-linking in mast cells (tryptase release, effective concentration for 50% inhibition [EC50] = 353 nmol/L) or basophils (histamine release, EC50 = 280 nmol/L), and by allergen (dust mite) in basophils (histamine release, EC50 = 490 nmol/L). R112 also blocks leukotriene C4 production and all proinflammatory cytokines tested. Its onset of action is immediate, and the inhibition is reversible. R112 is able to completely inhibit all three IgE-induced mast cell functions: degranulation, lipid mediator production, and cytokine production. R112 does not inhibit phosphorylation of the Lyn target Syk (Y352), but inhibits the phosphorylation of the Syk target LAT (Y191), indicating that Syk kinase is the primary target of R112. Most phosphorylation events downstream of Syk are inhibited with similar potency by R112. In vitro kinase assays do not always correlate with the corresponding activity inside cells. R112 inhibits the Lyn kinase in vitro assay with an IC50 of 0.3 μmol/L; however, as mentioned previously, in CHMCs (Cultured human mast cells), R112 does not inhibit the phosphorylation of Syk (Y352), and therefore most likely does not inhibit Lyn activity[1].

Chemical Information & Solubility

Molecular Weight 312.30 Formula

C16H13FN4O2
CAS No. 575474-82-7 SDF --
Smiles C1=CC(=CC(=C1)O)NC2=NC(=NC=C2F)NC3=CC(=CC=C3)O
Storage (From the date of receipt) 3 years -20°C powder

In vitro
Batch:

DMSO : 62 mg/mL ( (198.52 mM)； Moisture-absorbing DMSO reduces solubility. Please use fresh DMSO.)

Water : Insoluble

Ethanol : Insoluble


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In vivo
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Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid concentration mg/mL, Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug. )

Method for preparing in vivo formulation: Take μL DMSO master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O, mix and clarify.

Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.

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Tech Support

Answers to questions you may have can be found in the inhibitor handling instructions. Topics include how to prepare stock solutions, how to store inhibitors, and issues that need special attention for cell-based assays and animal experiments.

Handling Instructions

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