AS-604850
AS-604850
CAS: 648449-76-7
Molecular Formula: C11H5F2NO4S
AS-604850 - Names and Identifiers
AS-604850 - Physico-chemical Properties
| Molecular Formula | C11H5F2NO4S |
| Molar Mass | 285.22 |
| Density | 1.71 |
| Solubility | Soluble in DMSO (>10 mg/ml), water (<2 mg/ml), acetonitrile (6 mg/ml), methanol (9 mg/m |
| Appearance | solid |
| Color | off-white |
| pKa | 7.07±0.20(Predicted) |
| Storage Condition | 2-8°C |
| MDL | MFCD19705528 |
| Use | An ATP-competitive inhibitor of PI 3-kinase γ. |
| In vitro study | AS-604850 inhibits C5a-mediated PKB phosphorylation with an IC 50 of 10 μM in RAW264 mouse macrophages. AS-604850 blocks PKB phosphorylation induced by MCP-1 and has little or no effect after stimulation with CSF-1 in in primary monocytes from Pik3cg +/+ or Pik3cg –/– mice. AS-604850 (0-30 μM; 15 minutes; primary monocytes from Pik3cg +/+ mice) treatment inhibits MCP-1-mediated phosphorylation of PKB and its downstream substrates GSK3α andβ in a concentration-dependent manner. MCP-1-induced phosphorylation of p44/42 ERK (ERK1/2) MAPKs is also reduced, in a concentration dependent manner in primary monocytes from Pik3cg +/+ mice. Western Blot Analysis Cell Line: Primary monocytes from Pik3cg +/+ mice Concentration: 0 μM, 1 μM, 3 μM, 10 μM, 30 μM Incubation Time: 15 minutes Result: Inhibited MCP-1-mediated phosphorylation of PKB and its downstream substrates GSK3α andβ in a concentration-dependent manner. MCP-1-induced phosphorylation of p44/42 ERK (ERK1/2) MAPKs was also reduced, in a concentrationdependent manner in primary monocytes from Pik3cg +/+ mice. |
| In vivo study | AS-604850 (10-100 mg/kg; oral administration; for 4.5 or 4.25 hours; Balb/C or C3H mice) treatment reduces RANTES-induced peritoneal neutrophil recruitment with an ED 50 value 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. Animal Model: Balb/C or C3H mice with human recombinant RANTES or thioglycollate Dosage: 10 mg/kg, 30 mg/kg or 100 mg/kg Administration: Oral administration; for 4.5 or 4.25 hours Result: Reduced RANTES-induced peritoneal neutrophil recruitment with an ED 50 value of 42.4 mg/kg. In the thioglycollate-induced peritonitis model, resulted in a 31% reduction of neutrophil recruitment. |
AS-604850 - Risk and Safety
| Hazard Symbols | Xi - Irritant |
| Risk Codes | 43 - May cause sensitization by skin contact |
| Safety Description | 36/37 - Wear suitable protective clothing and gloves. |
| WGK Germany | 3 |
AS-604850 - Introduction
AS-604850 is a selective, ATP-competitive PI3Kγ inhibitor, IC50 is 250 nM, acting on PI3Kγ is more than 80 times more selective than acting on PI3Kδ/β, and acting on PI3Kγ is more selective than acting on PI3Kα 18 times higher selectivity.
Last Update：2022-10-16 17:41:44
AS-604850 - Reference Information
| biological activity | AS-604850 is an effective, selective and ATP competitive PI3Kγ inhibitor with IC50 value of 0.25 μM and Ki value of 0.18 μM. AS-604850 is an isoform selective inhibitor of PI3Kγ, and its selectivity to PI3Kγ is more than 30 times that of PI3Kδ/β and more than 18 times that of PI3Kα. |
| target | PI3Kγ 0.25 μM (IC 50 ) PI3Kγ 0.18 μM (Ki) PI3Kα 4.5 μM (IC 50 ) |
| in vitro study | AS-604850 inhibits C5a-mediated PKB phosphorylation with an IC 50 of 10 μ m in RAW264 mouse macrophages. AS-604850 blocks PKB phosphorylation induced by MCP-1 and has little or no effect after stimulation with CSF-1 in primary monocytes from Pik3cg +/+ or Pik3cg -/-mICE. AS-604850 (0-30 μ m; 15 minutes; primary monocytes from Pik3cg +/+ mice) treatment inhibits MCP-1-mediated phosphorylation of PKB and its downstream substrates GSK3α and β in a concentration-dependent manner. MCP-1-induced phosphorylation of p44/42 ERK (ERK1/2) MAPKs is also reduced, in a concentration dependent manner in primary monocytes from Pik3cg +/+ mice. Western Blot Analysis Cell Line: Primary monocytes from Pik3cg +/+ mice Concentration: 0 μM, 1 μM, 3 μM, 10 μM, 30 μM Incubation Time: 15 minutes Result: Inhibited MCP-1-mediated phosphorylation of PKB and its downstream substrates GSK3α and β in a concentration-dependent manner. MCP-1-induced phosphorylation of p44/42 ERK (ERK1/2) MAPKs was also reduced, in a concentrationdependent manner in primary monocytes from Pik3cg +/+ mice. |
| Cell Line: | Primary monocytes from Pik3cg +/+ mice |
| Concentration: | 0 μM, 1 μM, 3 μM, 10 μM, 30 μM |
| Incubation Time: | 15 minutes |
| Result: | Inhibited MCP-1-mediated phosphorylation of PKB and its downstream substrates GSK3α and β in a concentration-dependent manner. MCP-1-induced phosphorylation of p44/42 ERK (ERK1/2) MAPKs was also reduced, in a concentrationdependent manner in primary monocytes from Pik3cg +/+ mice. Reduced RANTES-induced peritoneal neutrophil recruitment with an ED 50 value of 42.4 mg/kg. In the thioglycollate-induced peritonitis model, resulted in a 31% reduction of neutrophil recruitment. |
| in vivo study | AS-604850 (10-100 mg/kg; oral administration; for 4.5 or 4.25 hours; Balb/C or C3H mice) treatment reduces RANTES-induced peritoneal neutrophil recruitment with an ED 50 value 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. Animal Model: Balb/C or C3H MICE with human recombinant RANTES or thioglycollate Dosage: 10 mg/kg, 30 mg/kg or 100 mg/kg Administration: Oral administration; For 4.5 or 4.25 hours result: reduced RANTES-induced peritoneal neutrophil recruitment with an ED 50 value of 42.4 mg/kg. In the thioglycollate-induced peritonitis model, resulted in a 31% reduction of neutrophil recruitment. |
| Animal Model: | Balb/C or C3H mice with human recombinant RANTES or thioglycollate |
| Dosage: | 10 mg/kg, 30 mg/kg or 100 mg/kg |
| Administration: | Oral administration; for 4.5 or 4.25 hours |
Last Update：2024-04-09 19:05:04
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