Syk Inhibitor II dihydrochloride dihydrate

Modify Date: 2024-02-04 05:54:07

Syk Inhibitor II dihydrochloride dihydrate Structure
Syk Inhibitor II dihydrochloride dihydrate structure
Common Name Syk Inhibitor II dihydrochloride dihydrate
CAS Number 1965323-05-0 Molecular Weight 449.26
Density N/A Boiling Point N/A
Molecular Formula C14H21Cl2F3N6O3 Melting Point N/A
MSDS N/A Flash Point N/A

 Use of Syk Inhibitor II dihydrochloride dihydrate


Syk Inhibitor II dihydrochloride dihydrate is a potent, high selective and ATP-competitive Syk inhibitor with an IC50 of 41 nM. Syk Inhibitor II dihydrochloride dihydrate inhibits 5-HT release from RBL-cells with an IC50 of 460 nM. Syk Inhibitor II dihydrochloride dihydrate shows less potent against other kinases and has anti-allergic effect[1].

 Names

Name Syk Inhibitor II dihydrochloride dihydrate

  Biological Activity

Description Syk Inhibitor II dihydrochloride dihydrate is a potent, high selective and ATP-competitive Syk inhibitor with an IC50 of 41 nM. Syk Inhibitor II dihydrochloride dihydrate inhibits 5-HT release from RBL-cells with an IC50 of 460 nM. Syk Inhibitor II dihydrochloride dihydrate shows less potent against other kinases and has anti-allergic effect[1].
Related Catalog
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) dihydrochloride dihydrate 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) dihydrochloride dihydrate 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.

 Chemical & Physical Properties

Molecular Formula C14H21Cl2F3N6O3
Molecular Weight 449.26