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R112

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Chemical Structure| 575474-82-7 同义名 : -
CAS号 : 575474-82-7
货号 : A325780
分子式 : C16H13FN4O2
纯度 : 98+%
分子量 : 312.298
MDL号 : MFCD12922519
存储条件：

粉末 Keep in dark place,Inert atmosphere,2-8°C

液体 -20°C:3-6个月-80°C:12个月
溶解度 :

DMSO: 55 mg/mL(176.11 mM)，配合低频超声助溶，注意：DMSO长时间开封后，会吸水并导致溶解能力下降，请避免使用长期开封的DMSO
动物实验配方：
生物活性
描述 Spleen tyrosine kinase (Syk) is a cytosolic non-receptor protein tyrosine kinase (PTK) and is mainly expressed in hematopoietic cells. Syk was recognized as a critical element in the B-cell receptor signaling pathway. Syk is also a key component in signal transduction from other immune receptors like Fc receptors and adhesion receptors[3]. 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[4]. 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. 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. R112 also blocks leukotriene C4 production and all proinflammatory cytokines tested. Its onset of action is immediate, and the inhibition is reversible[4].
实验方案
1mg 5mg 10mg

1 mM

5 mM

10 mM

3.20mL

0.64mL

0.32mL

16.01mL

3.20mL

1.60mL

32.02mL

6.40mL

3.20mL
参考文献

[1]Rossi AB, Herlaar E, et al. Identification of the Syk kinase inhibitor R112 by a human mast cell screen. J Allergy Clin Immunol. 2006 Sep;118(3):749-55.

[2]Meltzer EO, Berkowitz RB, 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):791-6.

[3]Liu D, Mamorska-Dyga A. Syk inhibitors in clinical development for hematological malignancies. J Hematol Oncol. 2017 Jul 28;10(1):145. doi: 10.1186/s13045-017-0512-1. PMID: 28754125; PMCID: PMC5534090.

[4]Rossi AB, Herlaar E, Braselmann S, Huynh S, Taylor V, Frances R, Issakani SD, Argade A, Singh R, Payan DG, Masuda ES. Identification of the Syk kinase inhibitor R112 by a human mast cell screen. J Allergy Clin Immunol. 2006 Sep;118(3):749-55. doi: 10.1016/j.jaci.2006.05.023. Epub 2006 Jul 28. PMID: 16950297.