AS-604850
Modify Date: 2024-01-04 19:57:47
AS-604850 structure
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Common Name | AS-604850 | ||
|---|---|---|---|---|
| CAS Number | 648449-76-7 | Molecular Weight | 285.224 | |
| Density | 1.7±0.1 g/cm3 | Boiling Point | N/A | |
| Molecular Formula | C11H5F2NO4S | Melting Point | N/A | |
| MSDS | USA | Flash Point | N/A | |
| Symbol |
GHS07 |
Signal Word | Warning | |
Use of AS-604850AS-604850 is a potent, selective and ATP-competitive PI3Kγ inhibitor with an IC50 value of 0.25 μM and a Ki value of 0.18 μM. AS-604850 shows isoform selective inhibitor of PI3Kγ with over 30-fold selectivity for PI3Kδ and β, and 18-fold selectivity over PI3Kα, respectively[1]. |
| Name | as-604850 |
|---|---|
| Synonym | More Synonyms |
| Description | AS-604850 is a potent, selective and ATP-competitive PI3Kγ inhibitor with an IC50 value of 0.25 μM and a Ki value of 0.18 μM. AS-604850 shows isoform selective inhibitor of PI3Kγ with over 30-fold selectivity for PI3Kδ and β, and 18-fold selectivity over PI3Kα, respectively[1]. |
|---|---|
| Related Catalog | |
| Target |
PI3Kγ:0.25 μM (IC50) PI3Kγ:0.18 μM (Ki) PI3Kα:4.5 μM (IC50) |
| In Vitro | AS-604850 inhibits C5a-mediated PKB phosphorylation with an IC50 of 10 μM in RAW264 mouse macrophages[1]. 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[1]. 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[1]. Western Blot Analysis[1] 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 | 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 ED50 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[1]. Animal Model: Balb/C or C3H mice with human recombinant RANTES or thioglycollate[1] 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 ED50 value of 42.4 mg/kg. In the thioglycollate-induced peritonitis model, resulted in a 31% reduction of neutrophil recruitment. |
| References |
| Density | 1.7±0.1 g/cm3 |
|---|---|
| Molecular Formula | C11H5F2NO4S |
| Molecular Weight | 285.224 |
| Exact Mass | 284.990723 |
| PSA | 89.93000 |
| LogP | 2.63 |
| Appearance of Characters | off-white |
| Index of Refraction | 1.658 |
| Storage condition | 2-8°C |
| Water Solubility | DMSO: >10mg/mL |
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Blockade of PI3Kgamma suppresses joint inflammation and damage in mouse models of rheumatoid arthritis.
Nat. Med. 11 , 936-943, (2005) Phosphoinositide 3-kinases (PI3K) have long been considered promising drug targets for the treatment of inflammatory and autoimmune disorders as well as cancer and cardiovascular diseases. But the lac... |
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