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Syk Inhibitor II dihydrochloride

Names

[ CAS No. ]:
227449-73-2

[ Name ]:
Syk Inhibitor II dihydrochloride

[Synonym ]:
Syk Inhibitor II

Biological Activity

[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.  

Chemical & Physical Properties

[ Molecular Formula ]:
C14H21Cl2F3N6O3

[ Molecular Weight ]:
449.25600

[ Exact Mass ]:
448.10000

[ PSA ]:
144.86000

[ LogP ]:
3.61220

Related Compounds