A selective blocker of spleen tyrosine kinase activity
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Alternative(s)
18202Syk Inhibitor II
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Syk Inhibitor II (hydrochloride)

Item No. 18805

Product Insert (PDF)Safety Data Sheet (SDS) (PDF)
Technical Information
Formal Name
2-[(2-aminoethyl)amino]-4-[[3-(trifluoromethyl)phenyl]amino]-5-pyrimidinecarboxamide, dihydrochloride
CAS Number
227449-73-2
Synonyms
  • Spleen Tyrosine Kinase Inhibitor II
Molecular Formula
C14H15F3N6O • 2HCl
Formula Weight
413.2
Purity
≥98%
Formulation (Request formulation change)
A crystalline solid
Solubility(Learn about Variance in Solubility)
DMF: 2 mg/mlDMSO: 30 mg/mlEthanol: 0.3 mg/mlPBS (pH 7.2): 10 mg/ml
λmax
255, 285 nm
SMILES
NCCNC1=NC(NC2=CC(C(F)(F)F)=CC=C2)=C(C(N)=O)C=N1.Cl.Cl
InChi Code
InChI=1S/C14H15F3N6O.2ClH/c15-14(16,17)8-2-1-3-9(6-8)22-12-10(11(19)24)7-21-13(23-12)20-5-4-18;;/h1-3,6-7H,4-5,18H2,(H2,19,24)(H2,20,21,22,23);2*1H
InChi Key
OWOVYLSSMDVDIW-UHFFFAOYSA-N
Shipping & Storage Information
Storage
-20°C
Shipping
Room temperature in continental US; may vary elsewhere
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    500 µg

    $132

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    Product Description

    Spleen tyrosine kinase (Syk) is a non-receptor tyrosine kinase that, upon phosphorylation, binds to immunoreceptor tyrosine-based activation motifs of FcRγ chains and mediates downstream signaling related to platelet function and inflammation. Syk inhibitor II is a cell-permeable, pyrimidine-carboxamide compound that selectively and reversibly blocks Syk (IC50 = 41 nM) in an ATP-competitive manner.1 It is much less potent against PKCε, PKCβII, ZAP-70, Btk, and Itk (IC50s = 5.1, 11, 11.2, 15.5, and 22.6 µM, respectively).1 Syk inhibitor II has been shown to prevent FcεRI-mediated 5-HT release in RBL-2H3 cells in vitro (IC50 = 460 nM) and to inhibit passive cutaneous anaphylaxis reactions in mice (ID50 = 13.2 mg/kg, s.c.).1

    WARNING This product is not for human or veterinary use.

    References & Product Citations
    Product Description References

    1. Hisamichi, J., Naito, R., Toyoshima, A., et al. Synthetic studies on novel Syk inhibitors. Part 1: Synthesis and structure-activity relationships of pyrimidine-5-carboxamide derivatives. Bioorg. Med. Chem. 13(16), 4936-4951 (2005).