AS-604850

Alias: AS604850; AS 604850; AS-604850
Cat No.:V0134 Purity: ≥98%
AS-604850 is a novel, potent, selective, and ATP-competitive inhibitor of PI3Kγ (phosphatidylinositol 3-kinase γ) with IC50 of 250 nM and aKi of 180 nM.
AS-604850 Chemical Structure CAS No.: 648449-76-7
Product category: PI3K
This product is for research use only, not for human use. We do not sell to patients.
Size Price Stock Qty
5mg
10mg
25mg
50mg
100mg
Other Sizes
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Purity & Quality Control Documentation

Purity: ≥98%

Product Description
AS-604850 is a novel, potent, selective, and ATP-competitive inhibitor of PI3Kγ (phosphatidylinositol 3-kinase γ) with IC50 of 250 nM and a Ki of 180 nM. With IC50s of 0.25 µM for PI3Kγ, >20 M for PI3Kδ and PI3Kβ, and 4.5 µM for PI3Kα, it displayed >80-fold selectivity for PI3Kγ over PI3Kδ/β, and 18-fold more selectivity for PI3Kγ over PI3Kα.
Biological Activity I Assay Protocols (From Reference)
Targets
PI3Kγ (IC50 = 0.25 μM); PI3Kγ (Ki = 0.18 μM); PI3Kα (IC50 = 4.5 μM)
ln 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 PI3Kδ and β, and 18-fold selectivity over PI3Kα. (PI3Kα: IC50 = 4.5 μM, PI3Kγ and β: IC50 > 20μM) With an IC50 of 10 μM, AS-604850 is able to prevent C5a-mediated PKB phosphorylation in RAW264 mouse macrophages. With an IC50 of 21 mM, AS-604850 inhibits MCP-1-mediated chemotaxis in Pik3cg +/+ monocytes in a concentration-dependent manner but has no effect on chemotaxis in Pik3cg -/- cells, demonstrating that AS-604850 functions through PI3Kγ.[1] In rat hepatocytes, AS-604850 reduces Akt-phosphorylation and apoptosis caused by glycochenodeoxycholate (GCDC). Apoptosis caused by bile salts in HepG2 Ntcp and Huh7-Ntcp cells is reduced by AS-604850. [2] Platelet-activating factor (PAF)-induced chemotactic responses of EoL-1 cells and blood eosinophils are suppressed by AS604850 in a concentration-dependent manner.[3]
ln Vivo
AS-604850 reduces RANTES-induced peritoneal neutrophil recruitment with a ED50 of 42.4 mg/kg. The oral administration of 10 mg/kg AS-604850 reduces neutrophil recruitment by 31% in the thioglycollate-induced peritonitis model.[1]
Enzyme 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. By first adding 250 g of Neomycin-coated Scintillation Proximity Assay (SPA) beads, the kinase reaction is stopped.
Cell Assay
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. Fluorescent staining is used to determine the morphology of apoptotic cells, and the percentage of apoptotic cells is expressed. In rat hepatocytes, caspase-3's 17 kDa proteolytic cleavage fragment is detected by immunoblotting, and in human cell lines, caspase-3/-7 activity is measured to confirm apoptosis. Actin immunoblotting is used to check for equal protein loading.
Animal Protocol
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
0, 1, 3, 10 or 30 mg/kg for RANTES, 10 mg/kg for thioglycollate
Oral administration 30 or 15 minutes before injection of RANTES or thioglycollate
References

[1]. Nat Med. 2005 Sep;11(9):936-43.

[2]. J Hepatol. 2010 Nov;53(5):918-26.

[3]. Int Immunopharmacol. 2010 Sep;10(9):1017-21.

These protocols are for reference only. InvivoChem does not independently validate these methods.
Physicochemical Properties
Molecular Formula
C11H5F2NO4S
Molecular Weight
285.2235
Exact Mass
284.99073
Elemental Analysis
C, 46.32; H, 1.77; F, 13.32; N, 4.91; O, 22.44; S, 11.24
CAS #
648449-76-7
Appearance
Solid powder
SMILES
C1=CC2=C(C=C1/C=C/3\C(=O)NC(=O)S3)OC(O2)(F)F
InChi Key
SRLVNYDXMUGOFI-XBXARRHUSA-N
InChi Code
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+
Chemical Name
(5E)-5-[(2,2-difluoro-1,3-benzodioxol-5-yl)methylidene]-1,3-thiazolidine-2,4-dione
Synonyms
AS604850; AS 604850; AS-604850
HS Tariff Code
2934.99.9001
Storage

Powder      -20°C    3 years

                     4°C     2 years

In solvent   -80°C    6 months

                  -20°C    1 month

Shipping Condition
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
Solubility Data
Solubility (In Vitro)
DMSO: ~57 mg/mL (~199.8 mM)
Water: <1 mg/mL
Ethanol: ~5 mg/mL (~17.5 mM)
Solubility (In Vivo)
0.5% CMC+0.25%Tween 80: 30mg/mL (Please use freshly prepared in vivo formulations for optimal results.)
Preparing Stock Solutions 1 mg 5 mg 10 mg
1 mM 3.5061 mL 17.5303 mL 35.0607 mL
5 mM 0.7012 mL 3.5061 mL 7.0121 mL
10 mM 0.3506 mL 1.7530 mL 3.5061 mL

*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.

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Note: Chemical formula is case sensitive: C12H18N3O4  c12h18n3o4
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In vivo Formulation Calculator (Clear solution)
Step 1: Enter information below (Recommended: An additional animal to make allowance for loss during the experiment)
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Calculation results

Working concentration mg/mL;

Method for preparing DMSO stock solution mg drug pre-dissolved in μL DMSO (stock solution concentration mg/mL). Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug.

Method for preparing in vivo formulation:Take μL DMSO stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O,mix and clarify.

(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
             (2) Be sure to add the solvent(s) in order.

Biological Data
  • Inhibitor of p110γ, AS604850, diminishes GCDC-induced PI3K activation and apoptosis but does not alter TUDC- and CPT-2-Me-cAMP induced signaling in hepatocytes. J Hepatol . 2010 Nov;53(5):918-26.
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