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AS-252424

Cayman Chemical Item Number 10009052

(CAS 900515-16-4)

AS-252424 (CAS 900515-16-4)

See more	Lipid Mediators (47) Inflammation (383) Signal Transduction (314)

Description

Phosphatidylinositol 3-kinase (PI3K) catalyzes the phosphorylation of Pl at the 3 position 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-252424 is a potent inhibitor of PI3K with selectivity for the γ isoform. It inhibits human recombinant PI3Kγ, α, β, and δ with IC₅₀ values of 30, 940, 20,000, and 20,000 nM respectively. ⁵ AS-252424 also inhibits C5a-mediated phosphorylation of Akt in RAW 264.7 macrophages with an IC₅₀ value of 0.23 µM. In a mouse model of peritonitis, AS-252424 inhibited neutrophil recruitment 35% at a dose of 10 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 21^st century'? Nat Rev Drug Discov 5 903-918 (2006).

5 Pomel, V., Klicic, J., Covini, D., et al. Furan-2-ylmethylene thiazolidinediones as novel, potent, and selective inhibitors of phosphoinositide 3-kinase γ. J Med Chem 49 3857-3871 (2006).

Formal Name	5-[5-(4-fluoro-2-hydroxy-phenyl)-furan-2-ylmethylene]-thiazolidine-2,4-dione
CAS Number	900515-16-4
Molecular Formula	C₁₄H₈FNO₄S
Formula Weight	305.3
Formulation	A crystalline solid
Purity	>95%
λ_max	408 nm
Stability	1 year
Storage	-20°C
Shipping	Room temperature in continental US; may vary elsewhere
SMILES	Copy SMILES to clipboard O=C(N([H])C(S/1)=O)C1=C\C2=CC=C(C3=C(O)C=C(F)C=C3)O2

Background Reading

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).

Pomel, V., Klicic, J., Covini, D., et al. Furan-2-ylmethylene thiazolidinediones as novel, potent, and selective inhibitors of phosphoinositide 3-kinase γ. J Med Chem 49 3857-3871 (2006).

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 21^st 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).

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AS-252424 is available in the following screening libraries:

Size	Price	Quantity	Subtotal
1 mg	$31.00		$0.00
5 mg	$140.00		$0.00
10 mg	$248.00		$0.00
25 mg	$543.00		$0.00
Bulk	Contact
		Cart Total	$0.00

Pricing updated 2012-02-10. 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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