|3,3'-((5-氟-2,4-嘧啶二基)二亚胺)二苯酚|CsnPharm

CAS No.: 575474-82-7

3,3'-((5-Fluoropyrimidine-2,4-diyl)bis(azanediyl))diphenol Catalog No. CSN18340

Synonyms: R112

R112, an ATP-competitive inhibitor, can inhibit Syk kinase with Ki of 96 nM.

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400-920-2911

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技术信息

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 K_i 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].
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.

实验方案

计算器摩尔计算器总药量计算器工作液计算器
储存液制备
- 1 mg
- 5 mg
- 10 mg
- 1 mM
- 3.2021 mL
- 16.0103 mL
- 32.0207 mL
- 5 mM
- 0.6404 mL
- 3.2021 mL
- 6.4041 mL
- 10 mM
- 0.3202 mL
- 1.6010 mL
- 3.2021 mL

技术信息

CAS号

575474-82-7

储存条件

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

液体: -20°C:3-6 月 -80°C:12月

分子式

C16H13FN4O2

运输

蓝冰

分子量

312.30

别名

R112

溶解度

DMSO	165.0 mg/mL (528.3 mM)
Water	150.0 mg/mL (480.3 mM) warming

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3,3'-((5-Fluoropyrimidine-2,4-diyl)bis(azanediyl))diphenol Catalog No. CSN18340

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