- 貨號 Cat. No.
- S2681
- 規格 Size
- 5~200mg
- 品牌 Brand
- Selleckchem
Description
AS-604850
AS-604850 is a selective, ATP-competitive PI3Kγ inhibitor with IC50 of 250 nM, over 80-fold selectivity for PI3Kγ than PI3Kδ/β, and 18-fold more selective for PI3Kγ than PI3Kα.
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10mM/1mLIn DMSO |
USD 151 |
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2mg |
USD 63 |
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5mg |
USD 126 |
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25mg |
USD 466 |
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100mg |
USD 1222 |
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Distributor Tel: +886-2-2827-1197jimmy@new.abscience.com.tw
Biological Activity
Description |
AS-604850 is a selective, ATP-competitive PI3Kγ inhibitor with IC50 of 250 nM, over 80-fold selectivity for PI3Kγ than PI3Kδ/β, and 18-fold more selective for PI3Kγ than PI3Kα. |
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Targets |
PI3Kγ |
PI3Kα |
PI3Kβ |
PI3Kδ |
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IC50 |
250 nM |
4.5 μM |
> 20 μM |
> 20 μM [1] |
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In vitro |
AS-604850 is ATP-competitive PI3Kγ inhibitor with Ki values of 0.18 μM. AS-604850 is isoform selective inhibitor of PI3Kγ with over 30-fold selectivity for PI3Kγ and β, and 18-fold selectivity over PI3Kα. (PI3Kα: IC50 = 4.5 μM, PI3Kγ and β: IC50 > 20μM) AS-604850 is capable of inhibiting C5a-mediated PKB phosphorylation in RAW264 mouse macrophages with an IC50 with 10 μM. AS-604850 blocks MCP-1-mediated chemotaxis in Pik3cg +/+monocytes in a concentration- dependent manner, with an IC50 of 21 mM, but dosnot affect chemotaxis in Pik3cg-/- cells, indicating that AS-604850 acts through PI3Kγ. [1] AS-604850 diminishes glycochenodeoxycholate (GCDC) induced Akt-phosphorylation and apoptosis in rat hepatocytes. AS-604850 diminishes bile salt-induced apoptosis in HepG2 Ntcp and Huh7-Ntcp cells. [2] AS604850 causes a concentration-dependent suppression of chemotactic responses of EoL-1 cells and blood eosinophils to platelet-activating factor (PAF). [3] |
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In vivo |
AS-604850 reduces RANTES-induced peritoneal neutrophil recruitment with a ED50 of 42.4 mg/kg. In the thioglycollate-induced peritonitis model, oral administration of 10 mg/kg AS-604850 results in a 31% reduction of neutrophil recruitment. [1] |
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Features |
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Protocol(Only for Reference)
Kinase Assay: [1]
In vitro PI3Kγ Kinase Assay |
Human PI3Kγ (100 ng) is incubated at RT with kinase buffer (10 mM MgCl2, 1 mM β-glycerophosphate, 1 mM DTT, 0.1 mM Na3VO4, 0.1% Na Cholate and 15 M ATP/100 nCi γ[33]ATP, final concentrations) and lipid vesicles containing 18 M PtdIns and 250 M of PtdSer (final concentrations), in the presence of AS-252424 or DMSO. Kinase reaction is stopped by adding 250 g of Neomycin-coated Scintillation Proximity Assay (SPA) beads and preceded. |
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Cell Assay: [2]
Cell lines |
HepG2 Ntcp and Huh7-Ntcp cells |
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Concentrations |
2.5 μM |
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Incubation Time |
2 - 4 hours |
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Method |
Hepatocyte cultures are treated with diluent (DMSO), 25 μM TLC, 250 μM TCDC, 50 μM GCDC, or 50 ng/ml Fas for 2-4 hours HepG2-Ntcp and Huh7-Ntcp cells are treated with DMSO, 20 μM TLC, 75 μM TCDC or GCDC, 200 μM etoposide or 200 ng/ml TNFa plus 28 ng/ml actinomycin D for 2-4 hours. The number of apoptotic cells is determined morphologically using fluorescent staining and expressed as % of cells. Apoptosis is confirmed in human cell lines by determination of caspase-3/-7 activity and in rat hepatocytes by detection of the 17 kDa proteolytic cleavage fragment of caspase-3 by immunoblotting; equal protein loading is monitored by immunoblotting for actin. |
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Animal Study: [1]
Animal Models |
RANTES (0.5 mg/kg in 200 ml saline) or thioglycollate (40 ml/kg) are intraperitoneally injected to C3H mice to induce peritonitis mouse models |
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Dosages |
0, 1, 3, 10 or 30 mg/kg for RANTES, 10 mg/kg for thioglycollate |
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Administration |
Oral administration 30 or 15 minutes before injection of RANTES or thioglycollate |
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Solubility |
0.5% CMC/0.25% Tween 80, 30 mg/mL |
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1
References
Download AS-604850 SDF
Molecular Weight (MW) |
285.22 |
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Formula |
C11H5F2NO4S
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CAS No. |
648449-76-7 |
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Storage |
3 years -20℃Powder |
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6 months-80℃in DMSO |
Syonnyms |
N/A |
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Solubility (25°C) * |
In vitro |
DMSO |
57 mg/mL (199 mM) |
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Water |
<1 mg/mL (<1 mM) |
Ethanol |
5 mg/mL (17 mM) |
In vivo |
0.5% CMC/0.25% Tween 80, |
30 mg/mL |
* <1 mg/ml means slightly soluble or insoluble.
* Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations. |
Chemical Name |
(Z)-5-((2,2-difluorobenzo[d][1,3]dioxol-5-yl)methylene)thiazolidine-2,4-dione |
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Stock Solution (1ml DMSO) |
1mM |
10mM |
20mM |
30mM |
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Mass(mg) |
0.28522 |
2.8522 |
5.7044 |
8.5566 |
Customer Reviews (1)
Click to enlarge |
Rating |
|
Source |
Dr. Zhang of Tianjin Medical University. AS-604850 purchased from Selleck |
Method |
Western blot |
Cell Lines |
A549 cells |
Concentrations |
0.01-10 μM |
Incubation Time |
3 h |
Results |
AS-604850 treatment resulted in a reduction of AKT phosphorylation. |
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