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 Details
| Alternative Name: | 2-[[7-(3,4-Dimethoxyphenyl)imidazo[1,2-c]pyrimidin-5-yl]amino]pyridine-3-carboxamide . HCl |
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| Formula: | C20H18N6O3 . HCl |
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| MW: | 390.4 . 36.5 |
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| CAS: | 648903-57-5 |
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| Purity: | ≥98% (HPLC(UV)) |
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| Identity: | Determined by MS. |
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| Appearance: | Yellow solid. |
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| Solubility: | Soluble in water (30mg/ml), DMSO (2mg/ml) or methanol (1mg/ml). |
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| Shipping: | Ambient Temperature |
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| Long Term Storage: | -20°C |
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| Handling: | Protect from light. Hygroscopic. |
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| Regulatory Status: | RUO - Research Use Only |
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Product Literature References
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;
Kinase inhibitors and airway inflammation: I.M. Adcock, et al.; Eur. J. Pharmacol.
533, 118 (2006),
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;
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;
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;
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