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Join us! · InformexUSA 2012 · New Orleans, Louisiana · February 14-17, 2012 · Booth 2514

AS-604850 Exclusive

Cayman Chemical Item Number 10010175

(CAS 648449-76-7)

AS-604850 (CAS 648449-76-7)

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Description

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

1 Rameh, L.E., and Cantley, L.C. The role of phosphoinositide 3-kinase lipid products in cell function. J Biol Chem 274 8347-8350 (1999).

2 Vivanco, I., and Sawyers, C.L. The phosphatidylinositol 3-kinase-AKT pathway in human cancer. Nat Rev 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. Nat Rev Drug Discov 4 988-1004 (2005).

4 Rückle, T., Schwarz, M.K., and Rommel, C. PI3Kγ inhibition: Towards an 'aspirin of the 21st century'? Nat Rev Drug Discov 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. Nat Med 11(9) 936-943 (2005).

Formal Name 5-​[(2,​2-​difluoro-​1,​3-​benzodioxol-​5-​yl)methylene]-​2,​4-​thiazolidinedione
CAS Number 648449-76-7
Molecular Formula C11H5F2NO4S
Formula Weight 285.2
Formulation A crystalline solid
Purity >98%
λmax 231, 328 nm
Stability 2 years
Storage -20°C
Shipping Room temperature in continental US; may vary elsewhere
SMILES
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O=C1NC(=O)​/C(=C\c2ccc3OC(F)​(F)​Oc3c2)​\S1

Background Reading

Camps, M., Rückle, T., Ji, H., et al. Blockade of PI3Kg suppresses joint inflammation and damage in mouse models of rheumatoid arthritis. Nat Med 11(9) 936-943 (2005).

Vivanco, I., and Sawyers, C.L. The phosphatidylinositol 3-kinase-AKT pathway in human cancer. Nat Rev Cancer 2 489-501 (2002).

Rückle, T., Schwarz, M.K., and Rommel, C. PI3Kγ inhibition: Towards an 'aspirin of the 21st century'? Nat Rev Drug Discov 5 903-918 (2006).

Hennessy, B.T., Smith, D.L., Ram, P.T., et al. Exploiting the PI3K/AKT pathway for cancer drug discovery. Nat Rev Drug Discov 4 988-1004 (2005).

Rameh, L.E., and Cantley, L.C. The role of phosphoinositide 3-kinase lipid products in cell function. J Biol Chem 274 8347-8350 (1999).

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AS-604850 is available in the following screening libraries:

Size Price Quantity Subtotal
1 mg $21.00 $0.00
5 mg $95.00 $0.00
10 mg $168.00 $0.00
25 mg $368.00 $0.00
Bulk Contact
Cart Total $0.00

This product is available in custom sizes and/or larger quantities.

Please contact our Sales Department for a quote or to purchase.

Pricing updated 2012-02-12. Prices are subject to change without notice.

To ask for assistance with one of our products please contact a Technical Support Scientist.

Warning This product is not for human or veterinary use.

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