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Sigma-Aldrich

Syk Inhibitor II

The Syk Inhibitor II, also referenced under CAS 227449-73-2, controls the biological activity of Syk. This small molecule/inhibitor is primarily used for Phosphorylation & Dephosphorylation applications.

Synonym(s):

Syk Inhibitor II, 2-(2-Aminoethylamino)-4-(3-trifluoromethylanilino)-pyrimidine-5-carboxamide, Dihydrochloride, Dihydrate

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About This Item

Empirical Formula (Hill Notation):
C14H15F3N6O · 2HCl · 2H2O
CAS Number:
227449-73-2
Molecular Weight:
449.26
UNSPSC Code:
12352200

Quality Level

100

Assay

≥95% (HPLC)

form

solid

manufacturer/tradename

Calbiochem®

storage condition

OK to freeze
desiccated (hygroscopic)
protect from light

color

off-white

solubility

DMSO: 100 mg/mL
water: 25 mg/mL

shipped in

ambient

storage temp.

2-8°C

InChI

1S/C14H15F3N6O.2ClH.2H2O/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;2*1H2

InChI key

LCACSMNPIITJGG-UHFFFAOYSA-N

General description

A cell-permeable pyrimidine-carboxamide compound that acts as a potent, selective, reversible, and ATP-competitive inhibitor of Syk (IC50 = 41 nM), while affecting PKCε, PKCβII, ZAP-70, Btk, and Itk only at much higher concentrations (IC50 = 5.1, 11, 11.2, 15.5, and 22.6 µM, respectively). Inhibits FcεRI-mediated 5-HT release in RBL-2H3 cells in vitro (IC50 = 460 nM) and passive cutaneous anaphylaxis (PCA) reaction in mice in vivo (ID50 = 13.2 mg/kg, s.c.).

Biochem/physiol Actions

Cell permeable: yes
Primary Target
Syk
Product competes with ATP.
Reversible: yes
Target IC50: 41 nM against Syk; 460 nM against FcεRI-mediated 5-HT release in RBL-2H3 cells in vitro

Packaging

Packaged under inert gas

Warning

Toxicity: Irritant (B)

Reconstitution

Following reconstitution, aliquot and freeze (-20°C). Stock solutions are stable for up to 6 months at -20°C.

Other Notes

Hisamichi, H., et al. 2005. Bioorg. Med. Chem.13, 4936.

Legal Information

CALBIOCHEM is a registered trademark of Merck KGaA, Darmstadt, Germany

Storage Class Code

11 - Combustible Solids

WGK

WGK 1

Certificates of Analysis (COA)

Search for Certificates of Analysis (COA) by entering the products Lot/Batch Number. Lot and Batch Numbers can be found on a product’s label following the words ‘Lot’ or ‘Batch’.

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