AS-605240 Inhibitor CAS No. 648450-29-7

Cat. No.	Name	Size	Price
KI1099	AS-605240	5 mg	$130
	AS-605240	10 mg	$200
	AS-605240	50 mg	$640
	AS-605240	100 mg	$1100

Chemical Characteristic

Product Name	AS-605240
CAS No.	648450-29-7
Molecular Weight	257.27
Formula	C₁₂H₇N₃O₂S
Chemical Name	(5Z)-5-(quinoxalin-6-ylmethylidene)-1,3-thiazolidine-2,4-dione
Smiles	S1C(=O)NC(=O)/C/1=C\c1cc2nccnc2cc1
Chemical Structure

Biological activities

AS-605240 is a potent and selective PI3Kγ inhibitor with an IC50 of 8 nM. AS-605240 also inhibits PI3Kα, PI3Kβ, and PI3Kδ with IC50 of 60, 270 and 300 nM, respectively. AS-605240 is an ATP-competitive PI3Kγ inhibitor with a Ki value of 7.8 nM. In RAW264 mouse macrophages, AS-605240 inhibits C5a-mediated PKB phosphorylation with an IC50 of 90 nM. In primary monocytes from Pik3cg^+/+ or Pik3cg^{????/sup> mice, AS-605240 (1 µM) blocks PKB phosphorylation induced by MCP-1 and has little or no effect after stimulation with CSF-1. Furthermore, in primary monocytes from Pik3cg^+/+ mice, AS-605240 reduces MCP-1-induced phosphorylation of p44/42 ERK (ERK1/2) MAPKs in a concentration-dependent manner. In a mouse model of collagen-induced arthritis in vivo, AS-605240 treatment (50 mg/kg) reduces synovium inflammation and cartilage erosion. In a mouse model of peritonitis induced by RANTES, AS-605240 reduces neutrophil chemotaxis with an ED50 of 9.1 mg/kg.^[1] In obese diabetic animal models, AS-605240 selectively blocks class IB PI3K signaling in cultured macrophages. Treatment with 10 mg/kg of AS-605240 lowers blood glucose levels, with an associated significant improvement of both insulin sensitivity and glucose tolerance without affecting body weight. Moreover, AS-605240 dose-dependently reduces the abundance of ATMs and the expression levels of macrophage markers in eWAT.^[2]}

Protocols

In vivo: AS-605240 is dissolved in 0.5% carboxymethylcellulose/0.25% Tween-20.^[1]

References

[1] Camps M, et al. Blockade of PI3Kgamma suppresses joint inflammation and damage in mouse models of rheumatoid arthritis. Nat Med. 2005, 11(9): 936-943. [2] Kobayashi N, et al. Blockade of class IB phosphoinositide-3 kinase ameliorates obesity-induced inflammation and insulin resistance. Proc Natl Acad Sci U S A. 2011, 108(14): 5753-5758.

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