AS-252424 |
| Catalog No.GC13901 |
PI3Kγ inhibitor,novel and potent
Products are for research use only. Not for human use. We do not sell to patients.
Cas No.: 900515-16-4
Sample solution is provided at 25 µL, 10mM.
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AS-252424 is a potent, selective and novel small-molecule PI3Kγ inhibitor (IC50= 30 nM)
PI3K (phosphatidylinositol-4,5-bisphosphate 3-kinase) is a family of enzymes involved in cellular functions such as cell growth, proliferation, differentiation, motility, survival and intracellular trafficking, which in turn are involved in cancer. It plays a key role in PI3K/Akt/mTOR pathway.
In THP-1 (human monocytic cell line), AS-252424 inhibited the phosphorylation of PKB/Akt due to MCP1 binding to the GPCR receptor CCR2 at lowest IC50 values of 0.4 μM. In primary monocytes and monocytic wild-type cell line THP-1, AS-252424 inhibited MCP-1-mediated chemotaxis in a concentration-dependent manner (IC50 value= 52 μM and 53 μM, respectively). [1] In Capan 1 and HPAF (pancreatic cancer cell lines), AS52424 specifically inhibited the cell proliferation. [2]
In a mouse model of thioglycollate-induced peritonitis, oral administration of AS-252424 at 10 mg/kg led to moderate reduction of neutrophil recruitment (35% ±14%). [1]
References:
1. Pomel V, Klicic J, Covini D et al. Furan-2-ylmethylene thiazolidinediones as novel, potent, and selective inhibitors of phosphoinositide 3-kinase gamma. J Med Chem. 2006 Jun 29;49(13):3857-71.
2. Edling CE, Selvaggi F, Buus R et al. Key role of phosphoinositide 3-kinase class IB in pancreatic cancer. Clin Cancer Res. 2010 Oct 15;16(20):4928-37.
Kinase experiment: | A PI3Kγ lipid kinase assay, based on the neomycin-coated scintillation proximity assay (SPA) bead technology, is performed in 384-well plates using ATP/[γ33P]ATP and PtdIns. Kinase assays for IC50 value determinations with PI3Kα, PI3Kβ, and PI3Kδ are carried out[1]. |
Cell experiment: | After 3 h of starvation in serum-free medium, Raw-264 macrophages are pretreated with inhibitors (e.g., AS-252424, 1 nM, 10 nM, 100 nM, 1 μM, 10 μM and 100 μM) or DMSO for 30 min and stimulated for 5 min with 50 nM C5a. PKB/Akt phosphorylation is monitored using phospho-Ser-473 Akt specific antibody and standard ELISA protocols[1]. |
Animal experiment: | Mice[1]PI3Kγ knockout (KO) mice are used. Oral administration of AS-252424 at 10 mg/kg is performed in PI3Kγ-deficient mice. |
References: [1]. Pomel V, et al. Furan-2-ylmethylene thiazolidinediones as novel, potent, and selective inhibitors of phosphoinositide 3-kinase gamma. J Med Chem. 2006 Jun 29;49(13):3857-71. | |
| Cas No. | 900515-16-4 | SDF | |
| Chemical Name | (5Z)-5-[[5-(4-fluoro-2-hydroxyphenyl)furan-2-yl]methylidene]-1,3-thiazolidine-2,4-dione | ||
| Canonical SMILES | C1=CC(=C(C=C1F)O)C2=CC=C(O2)C=C3C(=O)NC(=O)S3 | ||
| Formula | C14H8FNO4S | M.Wt | 305.28 |
| Solubility | ≥ 30.5mg/mL in DMSO | Storage | Store at -20°C |
| General tips | Please select the appropriate solvent to prepare the stock solution according to the
solubility of the product in different solvents; once the solution is prepared, please store it in
separate packages to avoid product failure caused by repeated freezing and thawing.Storage method
and period of the stock solution: When stored at -80°C, please use it within 6 months; when stored
at -20°C, please use it within 1 month. To increase solubility, heat the tube to 37°C and then oscillate in an ultrasonic bath for some time. |
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| Shipping Condition | Evaluation sample solution: shipped with blue ice. All other sizes available: with RT, or with Blue Ice upon request. | ||
| Prepare stock solution | |||
|
1 mg | 5 mg | 10 mg |
| 1 mM | 3.2757 mL | 16.3784 mL | 32.7568 mL |
| 5 mM | 0.6551 mL | 3.2757 mL | 6.5514 mL |
| 10 mM | 0.3276 mL | 1.6378 mL | 3.2757 mL |
Step 1: Enter information below (Recommended: An additional animal making an allowance for loss during the experiment)
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μL
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Calculation results:
Working concentration: mg/ml;
Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid 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 master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O, mix and clarify.
Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.
Note: 1. Please make sure the liquid is clear before adding the next solvent.
2. Be sure to add the solvent(s) in order. You must ensure that the solution obtained, in the previous addition, is a clear solution before proceeding to add the next solvent. Physical methods such as vortex, ultrasound or hot water bath can be used to aid dissolving.
3. All of the above co-solvents are available for purchase on the GlpBio website.
Quality Control & SDS
- View current batch:
- Purity: >99.00%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
- Datasheet
Average Rating: 5 (Based on Reviews and 1 reference(s) in Google Scholar.)
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