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ALX-270-479 Revised 29-Feb-08
BAY 61-3606 . hydrochloride
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SYNONYMS 2-[[7-(3,4-Dimethoxyphenyl)imidazo[1,2-c]pyrimidin-5-yl]amino]pyridine-3-carboxamide . HCl
PRODUCT LINE Signal Transduction
PRODUCT CATEGORY Tyrosine Kinase Inhibitors
Ordering Information
Product Numbers: Format: Size: Unit Price: Quantity: Add To Cart
ALX-270-479-M001   1 mg 40.00 USD Add To Cart
ALX-270-479-M005   5 mg 160.00 USD Add To Cart
ALX-270-479-M025   25 mg 560.00 USD Add To Cart
Product Specification
FORMULA: C20H18N6O3 . HCl
MW: 390.4 . 36.5
CAS NUMBER: 732938-37-8
PURITY: ≥98% (HPLC)
APPEARANCE: Yellow solid.
SOLUBILITY: Soluble in water (30mg/ml), DMSO (2mg/ml) or methanol (1mg/ml).
SHIPPING: AMBIENT
LONG TERM STORAGE: -20°C
HANDLING: Hygroscopic. Protect from light.

Product Description
Cell permeable, potent, ATP-competitive and reversible inhibitor of spleen tyrosine kinase (Syk) (IC50=10nM). Highly selective if compared to other kinases; shows no inhibitory effect against Btk, Fyn, Itk, Lyn, and Src up to concentrations of 4.7µM. Anti-inflammatory and orally active. Exhibits good in vivo efficacy in the treatment of various allergy and asthma conditions in rat models.
Product Specific Literature References
The orally available spleen tyrosine kinase inhibitor 2-[7-(3,4-dimethoxyphenyl)-imidazo[1,2-c]pyrimidin-5-ylamino]nicotinamide dihydrochloride (BAY 61-3606) blocks antigen-induced airway inflammation in rodents: N. Yamamoto, et al.; J. Pharmacol. Exp. Ther. 306, 1174 (2003) Abstract; Full Text
Modulation of the Fcepsilon receptor I signaling by tyrosine kinase inhibitors: search for therapeutic targets of inflammatory and allergy diseases: P. Luskova & P. Draber; Curr. Pharm. Des. 10, 1727 (2004) Abstract
A novel Syk kinase-selective inhibitor blocks antigen presentation of immune complexes in dendritic cells: K. Nakashima, et al.; Eur. J. Pharmacol. 505, 223 (2004) Abstract
Kinase inhibitors and airway inflammation: I.M. Adcock, et al.; Eur. J. Pharmacol. 533, 118 (2006) Abstract
Syk tyrosine kinase is linked to cell motility and progression in squamous cell carcinomas of the head and neck: S. Luangdilok, et al.; Cancer Res. 67, 7907 (2007) Abstract
 
 

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