Syk inhibitor II

Cas No.:	726695-51-8
Chemical Name:	2-[(2-aminoethyl)amino]-4-[[3-(trifluoromethyl)phenyl]amino]-5-pyrimidinecarboxamide
SMILES:	O=C(C1=CN=C(NCCN)N=C1NC2=CC=CC(C(F)(F)F)=C2)N
Formula:	C14H15F3N6O
M.Wt:	340.30
Purity:	>98%
Sotrage:	2 years -20°C Powder, 2 weeks 4°C in DMSO, 6 months -80°C in DMSO

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].
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 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].
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].
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.