PI3Kδ-IN-16
Based on 1 Customer Validation
PI3Kδ-IN-16 is a potent and selective PI3Kδ inhibitor with an IC50 value of 0.9 nM. PI3Kδ-IN-16 has a strong anti-proliferative effect on SU-DHL-6 cells, causing cell cycle arrest and inducing apoptosis. PI3Kδ-IN-16 tightly bins to PI3Kδ protein with a planar-shaped conformation. The kinase activity of PI3Kδ-IN-16 which is ~378-fold over PI3Kα, 412-fold over PI3Kβ, and 10-fold over PI3Kγ. PI3Kδ-IN-16 can be used for the study of hematologic malignancies.
For research use only. We do not sell to patients.
- Purity: 99.02%
- CAS No.: 2766437-35-6
- Formula: C22H26N6O2
- Molecular Weight:406.48
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Storage:
4°C, protect from light
* In solvent : -80°C, 6 months; -20°C, 1 month (protect from light)
To place orders, for customer services and technical support, please contact: MedChemExpress USA
Tel: 609-228-6898 E-mail: [email protected] [email protected]
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Biological Activity
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Chemical Information
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Solvent & Solubility
- Purity & Documentation
- References
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Help & FAQs
Biological Activity
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PI3Kδ 0.9 nM (IC50) |
PI3Kγ 8.7 nM (IC50) |
PI3Kα 340.1 nM (IC50) |
PI3Kβ 370.6 nM (IC50) |
PI3Kδ-IN-16 (Compound A10) demonstrates selective anti-proliferative activity against SU-DHL-6 cell line with an IC50 value of IC50 of 0.20 μM[1].
PI3Kδ-IN-16 (1-10 μM; 48 h) causes cell cycle arrest and induces apoptosis in SU-DHL-6 cells[1].
PI3Kδ-IN-16 (100-1000 nM; 8 h) significantly reduces the phosphorylation of Akt[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:SU-DHL-6 cell line
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Concentration:1 μM, 3.3 μM, 10 μM
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Incubation Time:24 h
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Result:Induced apoptosis of SU-DHL-6 cells in dose-dependent manner.
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Cell Line:SU-DHL-6 cell line
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Concentration:1 μM, 3.3 μM, 10 μM
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Incubation Time:24 h
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Result:Observed a markable increase in the number of cells in the G0/G1 phase.
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Cell Line:SU-DHL-6 cell line
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Concentration:100 nM, 1000 nM
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Incubation Time:8 h
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Result:Inhibited phosphorylated Akt in SU-DHL-6 cell line.
Chemical Information
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CAS No. 2766437-35-6
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Appearance Solid
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Molecular Weight 406.48
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Formula C22H26N6O2
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Color White to off-white
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SMILES
COC1=NC=C(C2=CC3=C(N=CN=C3N[C@@H](C)C(N4CCN(C)CC4)=O)C=C2)C=C1
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Shipping
Room temperature in continental US; may vary elsewhere.
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Storage
4°C, protect from light
* In solvent : -80°C, 6 months; -20°C, 1 month (protect from light)
Solvent & Solubility
DMSO : 76.92 mg/mL (189.23 mM; ultrasonic and adjust pH to 7 with 1 M HCl; 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 (protect from light). 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 (protect from light). 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: ≥ 2.5 mg/mL (6.15 mM); Clear solution
This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 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: ≥ 2.5 mg/mL (6.15 mM); Clear solution
This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 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:
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Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
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%DMSO +
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
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%+
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+%Tween-80 + +
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%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. * In solvent : -80°C, 6 months; -20°C, 1 month (protect from light)
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.
Purity & Documentation
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Data Sheet (273 KB)
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SDS (252 KB)
- English - EN (252 KB)
- Français - FR (252 KB)
- Deutsch - DE (252 KB)
- Norwegian - NO (252 KB)
- Español - ES (252 KB)
- Swedish - SV (252 KB)
- Italian - IT (252 KB)
- Korean - KR (252 KB)
- Portuguese - PT (252 KB)
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Handling Instructions (2659 KB)
References
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 (protect from light). 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 | 2.4601 mL | 12.3007 mL | 24.6015 mL | 61.5036 mL |
| 5 mM | 0.4920 mL | 2.4601 mL | 4.9203 mL | 12.3007 mL | |
| 10 mM | 0.2460 mL | 1.2301 mL | 2.4601 mL | 6.1504 mL | |
| 15 mM | 0.1640 mL | 0.8200 mL | 1.6401 mL | 4.1002 mL | |
| 20 mM | 0.1230 mL | 0.6150 mL | 1.2301 mL | 3.0752 mL | |
| 25 mM | 0.0984 mL | 0.4920 mL | 0.9841 mL | 2.4601 mL | |
| 30 mM | 0.0820 mL | 0.4100 mL | 0.8200 mL | 2.0501 mL | |
| 40 mM | 0.0615 mL | 0.3075 mL | 0.6150 mL | 1.5376 mL | |
| 50 mM | 0.0492 mL | 0.2460 mL | 0.4920 mL | 1.2301 mL | |
| 60 mM | 0.0410 mL | 0.2050 mL | 0.4100 mL | 1.0251 mL | |
| 80 mM | 0.0308 mL | 0.1538 mL | 0.3075 mL | 0.7688 mL | |
| 100 mM | 0.0246 mL | 0.1230 mL | 0.2460 mL | 0.6150 mL |
PI3Kδ-IN-16 Related Classifications
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