726695-51-8

726695-51-8 structure

Name: Syk inhibitor II
Chemical Name: Syk Inhibitor II
CAS Number: 726695-51-8
Molecular Formula: C₁₄H₁₅F₃N₆O
Molecular Weight: 340.304
Catalog: Signaling Pathways GPCR/G Protein 5-HT Receptor
Create Date: 2018-06-27 09:57:41
Modify Date: 2024-01-04 10:49:26
Syk Inhibitor II is a potent, high selective and ATP-competitive Syk inhibitor with an IC50 of 41 nM. Syk Inhibitor II inhibits 5-HT release from RBL-cells with an IC50 of 460 nM. Syk Inhibitor II shows less potent against other kinases and has anti-allergic effect[1].

Name	Syk Inhibitor II
Synonyms	5-Pyrimidinecarboxamide, 2-[(2-aminoethyl)amino]-4-[[3-(trifluoromethyl)phenyl]amino]- 2-[(2-Aminoethyl)amino]-4-{[3-(trifluoromethyl)phenyl]amino}-5-pyrimidinecarboxamide Syk Inhibitor II

Description	Syk Inhibitor II is a potent, high selective and ATP-competitive Syk inhibitor with an IC50 of 41 nM. Syk Inhibitor II inhibits 5-HT release from RBL-cells with an IC50 of 460 nM. Syk Inhibitor II shows less potent against other kinases and has anti-allergic effect[1].
Related Catalog	Signaling Pathways >> Protein Tyrosine Kinase/RTK >> Syk Research Areas >> Inflammation/Immunology Signaling Pathways >> GPCR/G Protein >> 5-HT Receptor Signaling Pathways >> Neuronal Signaling >> 5-HT Receptor
Target	serotonin:460 nM (IC50) Syk:41 nM (IC50) PKCε:5.1 μM (IC50) PKCβ2:11 μM (IC50) ZAP-70:11.2 μM (IC50) Btk:15.5 μM (IC50) Itk:22.6 μM (IC50)
In Vitro	Syk Inhibitor II (compound 9a) shows less potent against PKCε, PKCβ2, ZAP-70, Btk, and Itk with IC50 values of 5.1 µM, 11 µM, 11.2 µM, 15.5 µM, and 22.6 µM, respectively[1].
In Vivo	Syk Inhibitor II (Compound 9a; 10-100 mg/kg) is subcutaneously administered to mice 30 min before antigen challenge. Syk Inhibitor II inhibits the anaphylaxis reaction dose-dependently with an ID50 value of 13.2 mg/kg[1].
References	[1]. Hiroyuki Hisamichi, et al. Synthetic studies on novel Syk inhibitors. Part 1: Synthesis and structure-activity relationships of pyrimidine-5-carboxamide derivatives. Bioorg Med Chem. 2005 Aug 15;13(16):4936-51.