227449-73-2

227449-73-2 structure

Name: Syk Inhibitor II dihydrochloride
Chemical Name: 2-(2-aminoethylamino)-4-[3-(trifluoromethyl)anilino]pyrimidine-5-carboxamide,dihydrate,dihydrochloride
CAS Number: 227449-73-2
Molecular Formula: C₁₄H₂₁Cl₂F₃N₆O₃
Molecular Weight: 449.25600
Catalog: Signaling Pathways GPCR/G Protein 5-HT Receptor
Create Date: 2016-03-16 08:10:42
Modify Date: 2024-01-14 13:09:57
Syk Inhibitor II dihydrochloride is a potent, high selective and ATP-competitive Syk inhibitor with an IC50 of 41 nM. Syk Inhibitor II dihydrochloride inhibits 5-HT release from RBL-cells with an IC50 of 460 nM. Syk Inhibitor II dihydrochloride shows less potent against other kinases and has anti-allergic effect[1].

Name	2-(2-aminoethylamino)-4-[3-(trifluoromethyl)anilino]pyrimidine-5-carboxamide,dihydrate,dihydrochloride
Synonyms	Syk Inhibitor II

Description	Syk Inhibitor II dihydrochloride is a potent, high selective and ATP-competitive Syk inhibitor with an IC50 of 41 nM. Syk Inhibitor II dihydrochloride inhibits 5-HT release from RBL-cells with an IC50 of 460 nM. Syk Inhibitor II dihydrochloride 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	5-HT Receptor:460 nM (IC50)
In Vitro	Syk Inhibitor II (compound 9a) dihydrochloride 对 PKCε、PKCβ2、ZAP-70、Btk 和 Itk 的作用较弱，IC50 值分别为 5.1 µM、11 µM、11.2 µM、15.5 µM 和 22.6 µM[1]。
In Vivo	Syk Inhibitor II (Compound 9a; 10-100 mg/kg) dihydrochloride 在抗原攻击前 30 分钟皮下给药，以剂量依赖方式抑制过敏反应，ID50 值为13.2 mg/kg[1]。 Animal Model: ICR mice[1] Dosage: 10, 30, 100 mg/kg Administration: S.c.; 30 min before antigen challenge Result: Inhibited the anaphylaxis reaction dose-dependently with an ID50 value of 13.2 mg/kg.
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.