| Identification | Back Directory | [Name]
AS 604850 | [CAS]
648449-76-7 | [Synonyms]
CS-538
AS 604850
AS-604850;AS 604850
AS 604850 USP/EP/BP
PI 3-Kγ Inhibitor II
AS604850; AS 604850; AS-604850
PI 3-Kinase Inhibitor (AS604850)
PI 3-Kinase Inhibitor (AS604850) B-0302
PI 3-Kγ Inhibitor II - CAS 648449-76-7 - Calbiochem
5-(2,2-Difluoro-benzo[1,3]dioxol-5-ylmethylene)-thiazolidine-2,4-dione
5-[(2,2-Difluoro-1,3-benzodioxol-5-yl)methylene]thiazolidine-2,4-dione
2,4-Thiazolidinedione, 5-[(2,2-difluoro-1,3-benzodioxol-5-yl)methylene]-
(Z)-5-((2,2-difluorobenzo[d][1,3]dioxol-5-yl)methylene)thiazolidine-2,4-dione
PI3Kγ inhibitor, 5-(2,2-Difluoro-benzo[1,3]dioxol-5-ylmethylene)-thiazolidine-2,4-dione | [Molecular Formula]
C11H5F2NO4S | [MDL Number]
MFCD19705528 | [MOL File]
648449-76-7.mol | [Molecular Weight]
285.22 |
| Chemical Properties | Back Directory | [density ]
1.71 | [storage temp. ]
2-8°C | [solubility ]
DMSO: >10mg/mL | [form ]
solid | [pka]
7.07±0.20(Predicted) | [color ]
off-white | [InChI]
1S/C11H5F2NO4S/c12-11(13)17-6-2-1-5(3-7(6)18-11)4-8-9(15)14-10(16)19-8/h1-4H,(H,14,15,16)/b8-4- | [InChIKey]
SRLVNYDXMUGOFI-YWEYNIOJSA-N | [SMILES]
FC1(F)Oc2ccc(cc2O1)\C=C3/SC(=O)NC3=O |
| Hazard Information | Back Directory | [Description]
Phosphatidylinositol 3-kinase (PI3K) catalyzes the phosphorylation of PI at the three position of the inositol ring to produce the second messengers PtdIns-(3,4)-P2 and PtdIns-(3,4,5)-P3.1,2,3 PI3Kγ is a class 1B PI3K that is composed of a p110 catalytic subunit and a p101 or p84 regulatory subunit, whereas PI3Kα, β, and δ are class 1A enzymes composed of p110 and p85 subunits.4 AS-604850 is a selective, ATP-competitive inhibitor of PI3Kγ with IC50 values of 0.25, >20, >20, and 4.5 μM for the human recombinant γ, δ, β, and α isoforms, respectively.5 AS-604850 inhibited MCP-1-mediated monocyte chemotaxis with an IC50 value of 21 μM and reduced RANTES-induced peritoneal neutrophil recruitment in a murine model of leukocyte chemotaxis with an ED50 value of 42.4 mg/kg.5 | [Uses]
AS-604850 is a selective and ATP-competitive phosphoinositide 3-kinase gamma (PI3Kγ) inhibitor. | [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.
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| [IC 50]
PI3Kγ: 0.25 μM (IC50); PI3Kγ: 0.18 μM (Ki); PI3Kα: 4.5 μM (IC50) | [References]
1. camps m, rückle t, ji h et al. blockade of pi3k-gamma suppresses joint inflammation and damage in mouse models of rheumatoid arthritis. nat med. 2005 sep;11(9):936-43.2. hohenester s, gates a, wimmer r et al. phosphatidylinositol-3-kinase p110γ contributes to bile salt-induced apoptosis in primary rat hepatocytes and human hepatoma cells. j hepatol. 2010 nov;53(5):918-26. |
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