648449-76-7
648449-76-7 structure
- Name: AS-604850
- Chemical Name: as-604850
- CAS Number: 648449-76-7
- Molecular Formula: C11H5F2NO4S
- Molecular Weight: 285.224
- Catalog: Biochemical Inhibitor PI3K/Akt/mTOR inhibitor (PI3K/Akt/mTOR) PI3K inhibitor
- Create Date: 2016-08-13 01:10:24
- Modify Date: 2025-08-26 17:08:42
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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].
| Name | as-604850 |
|---|---|
| Synonyms |
5-(2,2-Difluoro-benzo[1,3]dioxol-5-ylmethylene)-thiazolidine-2,4-dione
2,4-Thiazolidinedione, 5-[(2,2-difluoro-1,3-benzodioxol-5-yl)methylene]-, (5Z)- 2,4-Thiazolidinedione, 5-[(2,2-difluoro-1,3-benzodioxol-5-yl)methylene]-, (5E)- (5Z)-5-[(2,2-Difluoro-1,3-benzodioxol-5-yl)methylene]-1,3-thiazolidine-2,4-dione (5E)-5-[(2,2-Difluoro-1,3-benzodioxol-5-yl)methylene]-1,3-thiazolidine-2,4-dione |
| 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 | off-white |
| Index of Refraction | 1.658 |
| Storage condition | 2-8°C |
| Water Solubility | DMSO: >10mg/mL |
| Symbol |
GHS07 |
|---|---|
| Signal Word | Warning |
| Hazard Statements | H317 |
| Precautionary Statements | P280 |
| Personal Protective Equipment | dust mask type N95 (US);Eyeshields;Faceshields;Gloves |
| Hazard Codes | Xi |
| Risk Phrases | 43 |
| Safety Phrases | 36/37 |
| RIDADR | NONH for all modes of transport |