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Syk inhibitor II

Names

[ CAS No. ]:
726695-51-8

[ Name ]:
Syk inhibitor II

[Synonym ]:
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

Biological Activity

[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.

Chemical & Physical Properties

[ Density]:
1.5±0.1 g/cm3

[ Boiling Point ]:
541.6±60.0 °C at 760 mmHg

[ Molecular Formula ]:
C14H15F3N6O

[ Molecular Weight ]:
340.304

[ Flash Point ]:
281.4±32.9 °C

[ Exact Mass ]:
340.125946

[ LogP ]:
1.25

[ Vapour Pressure ]:
0.0±1.4 mmHg at 25°C

[ Index of Refraction ]:
1.633

[ Storage condition ]:
-20℃

Related Compounds