| Identification | Back Directory | [Name]
2,4-Thiazolidinedione,5-(1,3-benzodioxol-5-ylmethylene)- | [CAS]
6318-41-8 | [Synonyms]
PI 3-Kγ Inhibitor VII - CAS 6318-41-8 - Calbiochem
2,4-Thiazolidinedione,5-(1,3-benzodioxol-5-ylmethylene)-
Inhibitor,PI3Kγ,inhibit,Phosphoinositide 3-kinase,AS 041164,AS-041164,anti-inflammatory,neutrophil,recruitment,AS041164,RANTES,PI3K | [Molecular Formula]
C11H7NO4S | [MDL Number]
MFCD18382117 | [MOL File]
6318-41-8.mol | [Molecular Weight]
249.24 |
| Chemical Properties | Back Directory | [density ]
1.595±0.06 g/cm3(Predicted) | [storage temp. ]
+2C to +8C | [solubility ]
Soluble in DMSO (up to 25 mg/ml). | [form ]
Yellow solid | [pka]
7.13±0.20(Predicted) | [color ]
Yellow | [Stability:]
Stable for 1 year from date of purchase as supplied. Solutions in DMSO may be stored at -20°C for up to 3 months. |
| Hazard Information | Back Directory | [Description]
The phosphatidylinositol 3-kinases (PI3Ks) are lipid and protein kinases involved in diverse biological processes, including cell growth, migration, and metabolism. AS-041164 is a potent inhibitor of PI3K with selectivity for the class IB isoform PI3Kγ (IC50 = 70 nM), compared to PI3Kα (IC50 = 240 nM), PI3Kβ (IC50 = 1.45 μM), and PI3Kδ (IC50 =1.70 μM). When tested at 1.0 μM, it shows little or no activity against 38 other common kinases. When given orally to mice, AS-041164 shows a pharmacokinetic profile that is similar to the general PI3K inhibitor LY294002 but is three times more potent (ED50 = 27.4 mg/kg for AS-041164 versus 81.6 mg/kg for LY294002) in blocking neutrophil recruitment induced by RANTES. | [Uses]
AS-041164 is a potent, selective and orally active PI3Kγ isoform inhibitor with an IC50 of 70 nM. AS-041164 shows less activity against PI3Kα, PI3Kβ, and PI3Kδ (IC50s of 240 nM, 1.45 μM, and 1.70 μM, respectively). AS-041164 has anti-inflammatory effects[1]. | [in vivo]
AS-041164 (10-100 mg/kg; oral administration; once) treatment results in the reduction of inflammatory swelling in the model of carrageenan-induced paw edema[1].
AS-041164 (3-100 mg/kg p.o.) treatment dose-dependently decreases r-h regulated on activation normal T cell expressed and secreted (RANTES)-induced neutrophil recruitment in mice. The ED50 value for AS-041164 is 27.35 mg/kg. AS-041164 blocks RANTES-induced chemotaxis and reduces the level of AKT phosphorylation[1]. | Animal Model: | Male Wistar rats (100-150 g) injected with carrageenan[1] | | Dosage: | 10 mg/kg, 30 mg/kg, 100 mg/kg | | Administration: | Oral administration; once | | Result: | Induced a significant reduction of paw thickness. |
| [IC 50]
PI3Kγ: 70 nM (IC50); PI3Kα: 240 nM (IC50); PI3Kβ: 1.4 μM (IC50); PI3Kδ: 1.7 μM (IC50) | [storage]
4°C, protect from light | [References]
1) Ferrandi et al. (2007) Phosphoinositide 3-kinase gamma inhibition plays a crucial role in early steps of inflammation by blocking neutrophil recruitment: J. Pharmacol. Exp. Ther. 322 923 |
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| Company Name: |
BOC Sciences
|
| Tel: |
1-631-485-4226; 16314854226 |
| Website: |
https://www.bocsci.com |
| Company Name: |
InvivoChem
|
| Tel: |
13549236410 |
| Website: |
https://www.invivochem.cn/ |
|