SF1670PTEN inhibitor, potent and specific CAS# 345630-40-2 |
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Quality Control & MSDS
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Chemical structure
3D structure
| Cas No. | 345630-40-2 | SDF | Download SDF |
| PubChem ID | 9926586 | Appearance | Powder |
| Formula | C19H17NO3 | M.Wt | 307.34 |
| Type of Compound | N/A | Storage | Desiccate at -20°C |
| Solubility | DMSO : ≥ 50 mg/mL (162.69 mM) H2O : < 0.1 mg/mL (insoluble) *"≥" means soluble, but saturation unknown. | ||
| Chemical Name | N-(9,10-dioxophenanthren-2-yl)-2,2-dimethylpropanamide | ||
| SMILES | CC(C)(C)C(=O)NC1=CC2=C(C=C1)C3=CC=CC=C3C(=O)C2=O | ||
| Standard InChIKey | VZQDDSYKVYARDW-UHFFFAOYSA-N | ||
| Standard InChI | InChI=1S/C19H17NO3/c1-19(2,3)18(23)20-11-8-9-13-12-6-4-5-7-14(12)16(21)17(22)15(13)10-11/h4-10H,1-3H3,(H,20,23) | ||
| General tips | For obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while.Stock solution can be stored below -20℃ for several months. We recommend that you prepare and use the solution on the same day. However, if the test schedule requires, the stock solutions can be prepared in advance, and the stock solution must be sealed and stored below -20℃. In general, the stock solution can be kept for several months. Before use, we recommend that you leave the vial at room temperature for at least an hour before opening it. |
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| About Packaging | 1. The packaging of the product may be reversed during transportation, cause the high purity compounds to adhere to the neck or cap of the vial.Take the vail out of its packaging and shake gently until the compounds fall to the bottom of the vial. 2. For liquid products, please centrifuge at 500xg to gather the liquid to the bottom of the vial. 3. Try to avoid loss or contamination during the experiment. |
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| Shipping Condition | Packaging according to customer requirements(5mg, 10mg, 20mg and more). Ship via FedEx, DHL, UPS, EMS or other couriers with RT, or blue ice upon request. | ||
| Description | PTPN2 and PTEN inhibitor (IC50values are 0.95 and 1.78 μM, respectively). Increases fMLP-elicited PIP3 signaling, Akt -phosphorylation and production of reactive oxygen species in neutrophils in vitro. Pretreatment of transfused neutrophils enhances chemotaxis to sites of bacterial infection and increases survival in neutropenic mice. Also inhibits CD45. |
SF1670 Dilution Calculator
SF1670 Molarity Calculator
| 1 mg | 5 mg | 10 mg | 20 mg | 25 mg | |
| 1 mM | 3.2537 mL | 16.2686 mL | 32.5373 mL | 65.0745 mL | 81.3431 mL |
| 5 mM | 0.6507 mL | 3.2537 mL | 6.5075 mL | 13.0149 mL | 16.2686 mL |
| 10 mM | 0.3254 mL | 1.6269 mL | 3.2537 mL | 6.5075 mL | 8.1343 mL |
| 50 mM | 0.0651 mL | 0.3254 mL | 0.6507 mL | 1.3015 mL | 1.6269 mL |
| 100 mM | 0.0325 mL | 0.1627 mL | 0.3254 mL | 0.6507 mL | 0.8134 mL |
| * Note: If you are in the process of experiment, it's necessary to make the dilution ratios of the samples. The dilution data above is only for reference. Normally, it's can get a better solubility within lower of Concentrations. | |||||
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SF1670 is a potent and specific inhibitor of PTEN [1].
Phosphatase and tensin homolog deleted on chromosome 10 (PTEN) is a phosphatidylinositol 3’-phosphatase that converts PtdIns(3,4,5)P3 to phosphatidylinositol 4,5-bisphosphate. PTEN functions as a tumor suppressor that is mutated in many cancers [1].
SF1670 is a potent and specific PTEN inhibitor. SF1670 bound to the active site of PTEN and increased PtdIns(3,4,5)P3 signaling in neutrophils. In human neutrophils, SF1670 significantly increased Akt phosphorylation stimulated by chemoattractant and specifically increased PtdIns(3,4,5)P3 signaling. SF1670 efficiently increased Akt phosphorylation at the concentration of 250nM. In mouse neutrophils, SF1670 also increased Akt phosphorylation and PtdIns(3,4,5)P3 signaling, which was mediated by the inhibition of PTEN activity. In neutrophils, SF1670 significantly increased reactive oxygen species (ROS) production induced by fMLP. Also, SF1670 increased neutrophil polarization induced by fMLP, which was necessary for the chemotactic migration and neutrophil recruitment to sites of inflammation [1].
In a mouse neutropenia-associated bacterial pneumonia model, SF1670 increased the bacteria-killing capability and relieved inflammation-associated lung damage [1].
Reference:
[1]. Li Y, Prasad A, Jia Y, et al. Pretreatment with phosphatase and tensin homolog deleted on chromosome 10 (PTEN) inhibitor SF1670 augments the efficacy of granulocyte transfusion in a clinically relevant mouse model. Blood, 2011, 117(24): 6702-6713.
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Pretreatment with phosphatase and tensin homolog deleted on chromosome 10 (PTEN) inhibitor SF1670 augments the efficacy of granulocyte transfusion in a clinically relevant mouse model.[Pubmed:21521784]
Blood. 2011 Jun 16;117(24):6702-13.
The clinical outcome of granulocyte transfusion therapy is often hampered by short ex vivo shelf life, inefficiency of recruitment to sites of inflammation, and poor pathogen-killing capability of transplanted neutrophils. Here, using a recently developed mouse granulocyte transfusion model, we revealed that the efficacy of granulocyte transfusion can be significantly increased by elevating intracellular phosphatidylinositol (3,4,5)-trisphosphate signaling with a specific phosphatase and tensin homolog deleted on chromosome 10 (PTEN) inhibitor SF1670. Neutrophils treated with SF1670 were much sensitive to chemoattractant stimulation. Neutrophil functions, such as phagocytosis, oxidative burst, polarization, and chemotaxis, were augmented after SF1670 treatment. The recruitment of SF1670-pretreated transfused neutrophils to the inflamed peritoneal cavity and lungs was significantly elevated. In addition, transfusion with SF1670-treated neutrophils led to augmented bacteria-killing capability (decreased bacterial burden) in neutropenic recipient mice in both peritonitis and bacterial pneumonia. Consequently, this alleviated the severity of and decreased the mortality of neutropenia-related pneumonia. Together, these observations demonstrate that the innate immune responses can be enhanced and the severity of neutropenia-related infection can be alleviated by augmenting phosphatidylinositol (3,4,5)-trisphosphate in transfused neutrophils with PTEN inhibitor SF1670, providing a therapeutic strategy for improving the efficacy of granulocyte transfusion.
