PIK-108
Based on 1 Customer Validation
PIK-108 is a non-ATP competitive, allosteric p110β/p110δ selective inhibitor.
Para uso exclusivo en investigación. No vendemos a pacientes.
- Pureza: 99.05%
- No. CAS: 901398-68-3
- Fòrmula: C22H24N2O3
- Peso molecular:364.44
-
Almacenamiento:Powder -20°C, 3 years ; In solvent -80°C, 6 months , -20°C, 1 month
To place orders, for customer services and technical support, please contact: MedChemExpress USA
Tel: 609-228-6898 E-mail: [email protected] [email protected]
-
Actividad biológica
-
Chemical Information
-
Solvente y solubilidad
- Pureza y Documentación
- Referencias
-
Help & FAQs
Actividad biológica
|
Cell Line
|
Type | Value | Description | References |
|---|---|---|---|---|
| PC-3 | IC50 |
3 nM
Compound: PIK-108
|
Inhibition of human PI3Kbeta-mediated Akt phosphorylation at Ser473 residue expressed in PTEN-deficient human PC3 cells by chemiluminescence assay
Inhibition of human PI3Kbeta-mediated Akt phosphorylation at Ser473 residue expressed in PTEN-deficient human PC3 cells by chemiluminescence assay
|
[PMID: 22524426] |
| PC-3 | IC50 |
3 nM
Compound: PIK-108
|
Inhibition of human PI3Kbeta-mediated Akt phosphorylation at T308 residue expressed in PTEN-deficient human PC3 cells after 2 hrs by Western blot analysis
Inhibition of human PI3Kbeta-mediated Akt phosphorylation at T308 residue expressed in PTEN-deficient human PC3 cells after 2 hrs by Western blot analysis
|
[PMID: 22524426] |
| PC-3 | IC50 |
3 nM
Compound: PIK-108
|
Inhibition of mTORC2-mediated Akt phosphorylation at Ser473 residue in PTEN-deficient human PC3 cells after 2 hrs by Western blot analysis
Inhibition of mTORC2-mediated Akt phosphorylation at Ser473 residue in PTEN-deficient human PC3 cells after 2 hrs by Western blot analysis
|
[PMID: 22524426] |
| Sf9 | IC50 |
>10000 nM
Compound: PIK-108
|
Inhibition of N-terminus poly-His tagged human PI3Kgamma expressed in baculovirus infected insect sf9 cells using PI(4,5)P2 as substrate preincubated with compound for 15 mins measured after 10 mins by HTRF assay
Inhibition of N-terminus poly-His tagged human PI3Kgamma expressed in baculovirus infected insect sf9 cells using PI(4,5)P2 as substrate preincubated with compound for 15 mins measured after 10 mins by HTRF assay
|
[PMID: 22524426] |
| Sf9 | IC50 |
658 nM
Compound: PIK-108
|
Inhibition of poly-His tagged human PI3Kdelta expressed in baculovirus infected insect sf9 cells coexpressing p85alpha using PI(4,5)P2 as substrate preincubated with compound for 15 mins measured after 10 mins by HTRF assay
Inhibition of poly-His tagged human PI3Kdelta expressed in baculovirus infected insect sf9 cells coexpressing p85alpha using PI(4,5)P2 as substrate preincubated with compound for 15 mins measured after 10 mins by HTRF assay
|
[PMID: 22524426] |
| Sf9 | IC50 |
>10000 nM
Compound: PIK-108
|
Inhibition of N-terminus poly-His tagged human PI3Kalpha expressed in baculovirus infected insect sf9 cells coexpressing p85alpha using PI(4,5)P2 as substrate preincubated with compound for 15 mins measured after 10 mins by HTRF assay
Inhibition of N-terminus poly-His tagged human PI3Kalpha expressed in baculovirus infected insect sf9 cells coexpressing p85alpha using PI(4,5)P2 as substrate preincubated with compound for 15 mins measured after 10 mins by HTRF assay
|
[PMID: 22524426] |
PIK-108 (0.1-10 μM; 1 hour) blocks phosphorylation of PKB/Akt[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
-
Cell Line:Glioma cell lines expressing wild-type PTEN
-
Concentration:0.1, 0.5, 1, 4, and 10 μM
-
Incubation Time:1 hour
-
Result:Showed variable inhibition of PKB/Akt phosphorylation but exhibited a trend toward reducing PKB/Akt phosphorylation more effectively in mutant PTEN-expressing cell lines than in wild-type PTEN-expressing cell lines.
Chemical Information
-
No. CAS 901398-68-3
-
Appearance Solid
-
Peso molecular 364.44
-
Fòrmula C22H24N2O3
-
Color White to off-white
-
SMILES
O=C1C=C(N2CCOCC2)OC3=C(C(NC4=CC=CC=C4)C)C=C(C)C=C13
-
Envío
Room temperature in continental US; may vary elsewhere.
-
Almacenamiento
Powder -20°C 3 years In solvent -80°C 6 months -20°C 1 month
Solvente y solubilidad
DMSO : 50 mg/mL (137.20 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
Select the appropriate dissolution method based on your experimental animal and administration route.
- For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
- To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for In Vivo experiments, it is recommended to prepare freshly and use it on the same day.
- The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.
Add each solvent one by one: 10% DMSO 40% PEG300 5% Tween-80 45% Saline
Solubility: ≥ 2.08 mg/mL (5.71 mM); Clear solution
This protocol yields a clear solution of ≥ 2.08 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (20.8 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.
Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
Add each solvent one by one: 10% DMSO 90% (20% SBE-β-CD in Saline)
Solubility: ≥ 2.08 mg/mL (5.71 mM); Clear solution
This protocol yields a clear solution of ≥ 2.08 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (20.8 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.
Preparation of 20% SBE-β-CD in Saline (4°C, storage for one week): 2 g SBE-β-CD powder is dissolved in 10 mL Saline, completely dissolve until clear.
Please enter the basic information of animal experiments:
-
-
-
-
Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
-
%DMSO +
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
-
%+
-
+%Tween-80 + +
-
%Saline +
The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).
Working solution concentration: 0.22 mg/mL
Method for preparing stock solution: mg drug dissolved in μL DMSO. Stock solution concentration: mg/mL.
1. Take μL DMSO stock solution;
2. Add μL .
μL , mix evenly;
3. Then add μL Tween 80, mix evenly;
4. Then add μL
Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.
Pureza y Documentación
-
Ficha de datos (276 KB)
-
SDS (251 KB)
- English - EN (251 KB)
- Français - FR (251 KB)
- Deutsch - DE (251 KB)
- Norwegian - NO (251 KB)
- Español - ES (251 KB)
- Swedish - SV (251 KB)
- Italian - IT (251 KB)
- Korean - KR (251 KB)
- Portuguese - PT (251 KB)
-
Instrucciones de manejo (2659 KB)
Referencias
[1]. Zachary A Knight, et al. A pharmacological map of the PI3-K family defines a role for p110alpha in insulin signaling. Cell. 2006 May 19;125(4):733-47. [Content Brief]
[2]. Jack S Chen, et al. Characterization of structurally distinct, isoform-selective phosphoinositide 3'-kinase inhibitors in combination with radiation in the treatment of glioblastoma. Mol Cancer Ther. 2008 Apr;7(4):841-50. [Content Brief]
Complete Stock Solution Preparation Table
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
| Optional Solvent | Concentration Solvent Mass | 1 mg | 5 mg | 10 mg | 25 mg |
|---|---|---|---|---|---|
| DMSO | 1 mM | 2.7439 mL | 13.7197 mL | 27.4394 mL | 68.5984 mL |
| 5 mM | 0.5488 mL | 2.7439 mL | 5.4879 mL | 13.7197 mL | |
| 10 mM | 0.2744 mL | 1.3720 mL | 2.7439 mL | 6.8598 mL | |
| 15 mM | 0.1829 mL | 0.9146 mL | 1.8293 mL | 4.5732 mL | |
| 20 mM | 0.1372 mL | 0.6860 mL | 1.3720 mL | 3.4299 mL | |
| 25 mM | 0.1098 mL | 0.5488 mL | 1.0976 mL | 2.7439 mL | |
| 30 mM | 0.0915 mL | 0.4573 mL | 0.9146 mL | 2.2866 mL | |
| 40 mM | 0.0686 mL | 0.3430 mL | 0.6860 mL | 1.7150 mL | |
| 50 mM | 0.0549 mL | 0.2744 mL | 0.5488 mL | 1.3720 mL | |
| 60 mM | 0.0457 mL | 0.2287 mL | 0.4573 mL | 1.1433 mL | |
| 80 mM | 0.0343 mL | 0.1715 mL | 0.3430 mL | 0.8575 mL | |
| 100 mM | 0.0274 mL | 0.1372 mL | 0.2744 mL | 0.6860 mL |
PIK-108 Related Classifications
HY-111184 Related Classifications
Powered by Bioz