10010175 AS-604850
(CAS 648449-76-7)
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Phosphatidylinositol 3-kinase (PI3K) catalyzes the phosphorylation of PI at the three position of the inositol ring to produce the second messengers PtdIns-(3,4)-P2 and PtdIns-(3,4,5)-P3.1,2,3 PI3Kγ is a class 1B PI3K that is composed of a p110 catalytic subunit and a p101 or p84 regulatory subunit, whereas PI3Kα, β, and δ are class 1A enzymes composed of p110 and p85 subunits.4 AS-604850 is a selective, ATP-competitive inhibitor of PI3Kγ with IC50 values of 0.25, >20, >20, and 4.5 µM for the human recombinant γ, δ, β, and α isoforms, respectively.5 AS-604850 inhibited MCP-1-mediated monocyte chemotaxis with an IC50 value of 21 µM and reduced RANTES-induced peritoneal neutrophil recruitment in a murine model of leukocyte chemotaxis with an ED50 value of 42.4 mg/kg.5
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1
Rameh, L.E., Cantley, L.C. The role of phosphoinositide 3-kinase lipid products in cell function. J Biol Chem 274 8347-8350 (1999).
2
Vivanco, I., Sawyers, C.L. The phosphatidylinositol 3-kinase-AKT pathway in human cancer. Nature Reviews Cancer 2 489-501 (2002).
3
Hennessy, B.T., Smith, D.L., Ram, P.T., et al. Exploiting the PI3K/AKT pathway for cancer drug discovery. Nature Reviews Drug Discovery 4 988-1004 (2005).
4
Rückle, T., Schwarz, M.K., Rommel, C. PI3Kγ inhibition: Towards an 'aspirin of the 21st century'?. Nature Reviews Drug Discovery 5 903-918 (2006).
5
Camps, M., Rückle, T., Ji, H., et al. Blockade of PI3Kg suppresses joint inflammation and damage in mouse models of rheumatoid arthritis. Nature Med 11(9) 936-943 (2005).
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Pricing updated 2010-03-19.
Prices are subject to change without notice.
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Stability of this item is suitable for room temperature overnight shipping. If shipment on ice is desired, it must be requested when the order is placed.
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