Leniolisib
Based on 1 publication(s) in Google Scholar
Leniolisib (CDZ173) is a potent and selective PI3Kδ inhibitor. Leniolisib has the potential for immunodeficiency disorders treatment.
Para uso exclusivo en investigación. No vendemos a pacientes.
- Pureza: 99.38%
- No. CAS: 1354690-24-6
- Fòrmula: C21H25F3N6O2
- Peso molecular:450.46
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Almacenamiento:Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 2 years , -20°C, 1 year
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Actividad biológica
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Chemical Information
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Solvente y solubilidad
- Pureza y Documentación
- Referencias
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Help & FAQs
Publications Citing Use of MedChemExpress (MCE) Leniolisib
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Actividad biológica
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PI3Kδ 11 nM (IC50) |
PI3Kα 280 nM (IC50) |
PI3Kβ 480 nM (IC50) |
PI3Kγ 2.57 μM (IC50) |
DNA-PK 880 nM (IC50) |
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Cell Line
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Type | Value | Description | References |
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| DOHH-2 | IC50 |
29.2 μM
Compound: Fig 1, Cpd 9; CDZ173
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Antiproliferative activity against human DOHH-2 cells assessed as cell growth inhibition incubated for 96 hrs by cell titer glo assay
Antiproliferative activity against human DOHH-2 cells assessed as cell growth inhibition incubated for 96 hrs by cell titer glo assay
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[PMID: 35609190] |
| JeKo-1 | IC50 |
31.66 μM
Compound: Fig 1, Cpd 9; CDZ173
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Antiproliferative activity against human JeKo-1 cells assessed as cell growth inhibition incubated for 96 hrs by cell titer glo assay
Antiproliferative activity against human JeKo-1 cells assessed as cell growth inhibition incubated for 96 hrs by cell titer glo assay
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[PMID: 35609190] |
| Pfeiffer | IC50 |
3.75 μM
Compound: Fig 1, Cpd 9; CDZ173
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Antiproliferative activity against human Pfeiffer cells assessed as cell growth inhibition incubated for 96 hrs by cell titer glo assay
Antiproliferative activity against human Pfeiffer cells assessed as cell growth inhibition incubated for 96 hrs by cell titer glo assay
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[PMID: 35609190] |
| Rec1 | IC50 |
1.28 μM
Compound: Fig 1, Cpd 9; CDZ173
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Antiproliferative activity against human REC1 cells assessed as cell growth inhibition incubated for 96 hrs by cell titer glo assay
Antiproliferative activity against human REC1 cells assessed as cell growth inhibition incubated for 96 hrs by cell titer glo assay
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[PMID: 35609190] |
| SUD4 | IC50 |
8.25 μM
Compound: Fig 1, Cpd 9; CDZ173
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Antiproliferative activity against human SU-DHL-4 cells assessed as cell growth inhibition incubated for 96 hrs by cell titer glo assay
Antiproliferative activity against human SU-DHL-4 cells assessed as cell growth inhibition incubated for 96 hrs by cell titer glo assay
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[PMID: 35609190] |
| SU-DHL-6 | IC50 |
0.77 μM
Compound: Fig 1, Cpd 9; CDZ173
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Antiproliferative activity against human SU-DHL-6 cells assessed as cell growth inhibition incubated for 96 hrs by cell titer glo assay
Antiproliferative activity against human SU-DHL-6 cells assessed as cell growth inhibition incubated for 96 hrs by cell titer glo assay
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[PMID: 35609190] |
| Z-138 | IC50 |
31.19 μM
Compound: Fig 1, Cpd 9; CDZ173
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Antiproliferative activity against human Z138 cells assessed as cell growth inhibition incubated for 96 hrs by cell titer glo assay
Antiproliferative activity against human Z138 cells assessed as cell growth inhibition incubated for 96 hrs by cell titer glo assay
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[PMID: 35609190] |
Expression of APDS mutant p110δ in cell lines and patient-derived lymphocytes lead to increased pathway activity, measured as phosphorylation of AKT or S6, which is suppressed by leniolisib in a concentration dependent way[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
| NCT Number | Sponsor | Condition | Start Date |
Phase
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|---|---|---|---|---|
| NCT01329991 | Plexxikon| | 2011-05 | PHASE1 |
Chemical Information
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No. CAS 1354690-24-6
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Appearance Solid
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Peso molecular 450.46
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Fòrmula C21H25F3N6O2
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Color White to off-white
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SMILES
CCC(N1C[C@@H](NC2=C(CN(C3=CC(C(F)(F)F)=C(OC)N=C3)CC4)C4=NC=N2)CC1)=O
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Synonyms
CDZ173
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Envío
Room temperature in continental US; may vary elsewhere.
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Almacenamiento
Powder -20°C 3 years 4°C 2 years In solvent -80°C 2 years -20°C 1 year
Publications (1)
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Journal Impact Factor
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Most Recent
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Mol Syst Biol
Illuminating phenotypic drug responses of sarcoma cells to kinase inhibitors by phosphoproteomics. [Abstract]2024 Jan;20(1):28-55. PMID: 38177929
Solvente y solubilidad
DMSO : 100 mg/mL (222.00 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, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.
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, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.
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 (5.55 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 (5.55 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.
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
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Ficha de datos (280 KB)
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SDS (393 KB)
- English - EN (393 KB)
- Français - FR (393 KB)
- Deutsch - DE (393 KB)
- Norwegian - NO (393 KB)
- Español - ES (393 KB)
- Swedish - SV (393 KB)
- Italian - IT (393 KB)
- Korean - KR (393 KB)
- Portuguese - PT (393 KB)
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Instrucciones de manejo (2659 KB)
Referencias
[1]. Rao V, et al. Effective 'Activated PI3Kd Syndrome' -targeted therapy with PI3Kd inhibitor leniolisib. The New England journal of medicine: NEJM. ISSN 0028-4793; 1533-4406 [Content Brief]
[2]. Hoegenauer K, et al. Discovery of CDZ173 (Leniolisib), Representing a Structurally Novel Class of PI3K Delta-Selective Inhibitors. ACS Med Chem Lett. 2017 Aug 25;8(9):975-980. [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, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.
| Optional Solvent | Concentration Solvent Mass | 1 mg | 5 mg | 10 mg | 25 mg |
|---|---|---|---|---|---|
| DMSO | 1 mM | 2.2200 mL | 11.0998 mL | 22.1995 mL | 55.4988 mL |
| 5 mM | 0.4440 mL | 2.2200 mL | 4.4399 mL | 11.0998 mL | |
| 10 mM | 0.2220 mL | 1.1100 mL | 2.2200 mL | 5.5499 mL | |
| 15 mM | 0.1480 mL | 0.7400 mL | 1.4800 mL | 3.6999 mL | |
| 20 mM | 0.1110 mL | 0.5550 mL | 1.1100 mL | 2.7749 mL | |
| 25 mM | 0.0888 mL | 0.4440 mL | 0.8880 mL | 2.2200 mL | |
| 30 mM | 0.0740 mL | 0.3700 mL | 0.7400 mL | 1.8500 mL | |
| 40 mM | 0.0555 mL | 0.2775 mL | 0.5550 mL | 1.3875 mL | |
| 50 mM | 0.0444 mL | 0.2220 mL | 0.4440 mL | 1.1100 mL | |
| 60 mM | 0.0370 mL | 0.1850 mL | 0.3700 mL | 0.9250 mL | |
| 80 mM | 0.0277 mL | 0.1387 mL | 0.2775 mL | 0.6937 mL | |
| 100 mM | 0.0222 mL | 0.1110 mL | 0.2220 mL | 0.5550 mL |
Leniolisib Related Classifications
HY-17635 Related Classifications
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