| Size | Price | Stock | Qty |
|---|---|---|---|
| 10mg |
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| 25mg |
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| 50mg |
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| 100mg |
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| 250mg |
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| 500mg |
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| Other Sizes |
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Purity: ≥98%
| Targets |
PI3Kγ (IC50 = 0.25 μM); PI3Kγ (Ki = 0.18 μM); PI3Kα (IC50 = 4.5 μM)
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|---|---|
| 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]
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| 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]
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| 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.
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| 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.
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| 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 |
| Molecular Formula |
C11H5F2NO4S
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|---|---|
| Molecular Weight |
285.2235
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| Exact Mass |
284.99
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| Elemental Analysis |
C, 46.32; H, 1.77; F, 13.32; N, 4.91; O, 22.44; S, 11.24
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| CAS # |
648449-76-7
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| Related CAS # |
648449-76-7
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| PubChem CID |
11492951
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| Appearance |
White to off-white solid powder
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| Density |
1.7±0.1 g/cm3
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| Index of Refraction |
1.658
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| LogP |
2.63
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| Hydrogen Bond Donor Count |
1
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| Hydrogen Bond Acceptor Count |
7
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| Rotatable Bond Count |
1
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| Heavy Atom Count |
19
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| Complexity |
468
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| Defined Atom Stereocenter Count |
0
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| SMILES |
S1C(N([H])C(/C/1=C(\[H])/C1C([H])=C([H])C2=C(C=1[H])OC(O2)(F)F)=O)=O
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| InChi Key |
SRLVNYDXMUGOFI-XBXARRHUSA-N
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| 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+
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| Chemical Name |
(5E)-5-[(2,2-difluoro-1,3-benzodioxol-5-yl)methylidene]-1,3-thiazolidine-2,4-dione
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| Synonyms |
AS604850; AS 604850; AS-604850
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| HS Tariff Code |
2934.99.9001
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| 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)
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| Solubility (In Vitro) |
DMSO: ~57 mg/mL (~199.8 mM)
Water: <1 mg/mL Ethanol: ~5 mg/mL (~17.5 mM) |
|---|---|
| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.08 mg/mL (7.29 mM) (saturation unknown) in 10% DMSO + 40% PEG300 + 5% Tween80 + 45% Saline (add these co-solvents sequentially from left to right, and one by one), clear solution.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 20.8 mg/mL clear DMSO stock solution to 400 μL PEG300 and mix evenly; then add 50 μL Tween-80 to the above solution and mix evenly; then add 450 μL normal saline to adjust the volume to 1 mL. Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH₂ O to obtain a clear solution. Solubility in Formulation 2: ≥ 2.08 mg/mL (7.29 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one), clear solution. For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 20.8 mg/mL clear DMSO stock solution to 900 μL of corn oil and mix evenly. View More
Solubility in Formulation 3: 0.5% CMC+0.25%Tween 80: 30mg/mL |
| 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.
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.
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