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Product Details

AS-605240 | PI 3-Kinase inhibitor

AS-605240 (648450-29-7) is a potent and selective inhibitor of PI 3-kinase γ (PI 3-Kγ), IC50 = 8 nM displaying 30-fold selectivity over PI 3-Kδ and PI 3-Kβ and 7.5-fold selectivity over PI 3-Kα1. Suppresses joint inflammation in two distinct mouse models1. Ameliorates surgical brain injury2, colitis3, intimal hyperplasia-induced inflammatory processes4 and renal injury/fibrosis5 in rodent models. Orally active.

References/Citations

1) Camps et al. (2005), Blockade of PI3Kgamma suppresses joint inflammation and damage in mouse models of rheumatoid arthritis; Nature Med., 11 936
2) Huang et al. (2015), Phosphoinositide 3-Kinase Gamma Contributes to Neuroinflammation ina Rat Model of Surgical Brain Injury; J. Neurosci., 35 10390
3) Peng et al. (2010), Inhibition of phosphoinositide 3-kinase ameliorates dextran sodium sulfate-induced colitis in mice; J. Pharmacol. Exp. Ther., 332 46
4) Smimova et al. (2014), Targeting PI3Kγ activity decreases vascular trauma-induced intimal hyperplasia through modulation of the Th1 response; J. Exp. Med., 211 1779
5) Yu et al. (2018), A blockade of PI3Kγ signaling effectively mitigates angiotensin II-induced renal injury and fibrosis in a mouse model; Sci. Rep., 8 10988

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Catalog#  10-2575-0005

$50.00
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Please note that we do not sell to individuals and that all orders placed by non-research organizations will incur a $20 restocking/refund fee.
 
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CAS:
348450-29-7
Catalog Number:
10-2575
Activity:
PI 3-Kinase inhibitor
Chemical Name:
5-(6-Quinoxalinylmethylene)-2,4-thiazolidine-2,4-dione
Molecular Weight:
257.27
Molecular Formula:
C12H7N2O3
Solubility:
Soluble in DMSO (up to 1.5 mg/ml with warming)
Physical Properties:
Red solid
Purity:
98% by TLC
NMR (Conforms)
Storage Temperature:
-20°C (des.)
Stability:
Stable for 2 years as supplied. Solutions in DMSO may be stored at -20°C for up to 1 month.
Shipping Code:
RT
Materials provided by Focus Biomolecules are for laboratory research use only and are not intended for human or veterinary applications.

Focus BiomoleculesPlymouth Meeting, PA USA1-855-FOCUS21

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