Leniolisib-d5
Based on 1 Customer Validation
Leniolisib-d5 is a deuterated labeled Leniolisib. Leniolisib (CDZ173) is a potent and selective PI3Kδ inhibitor. Leniolisib has the potential for immunodeficiency disorders treatment.
For research use only. We do not sell to patients.
- Purity: 98.78%
- Formula: C21H20D5F3N6O2
- Molecular Weight:455.49
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Storage:Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 6 months , -20°C, 1 month
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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
Stable heavy isotopes of hydrogen, carbon, and other elements have been incorporated into drug molecules, largely as tracers for quantitation during the drug development process. Deuteration has gained attention because of its potential to affect the pharmacokinetic and metabolic profiles of drugs[1].
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[2].
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.
1. This compound can be used as a tracer
2. This compound can be used as an internal standard for quantitative analysis by NMR, GC-MS, or LC-MS.
Chemical Information
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Unlabeled Cas 1354690-24-6
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Appearance Solid
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Molecular Weight 455.49
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Formula C21H20D5F3N6O2
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Color White to off-white
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SMILES
COC1=C(C(F)(F)F)C=C(N2CC(C(N[C@H]3CCN(C(C([2H])([2H])C([2H])([2H])[2H])=O)C3)=NC=N4)=C4CC2)C=N1
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Synonyms
CDZ173-d5
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Shipping
Room temperature in continental US; may vary elsewhere.
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Storage
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month
Solvent & Solubility
DMSO : 100 mg/mL (219.54 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)
Purity & Documentation
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Data Sheet (281 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)
- Portuguese - PT (393 KB)
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Handling Instructions (2659 KB)
References
[1]. Russak EM, et al. Impact of Deuterium Substitution on the Pharmacokinetics of Pharmaceuticals. Ann Pharmacother. 2019 Feb;53(2):211-216. [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]
[3]. 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]
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 | 2.1954 mL | 10.9772 mL | 21.9544 mL | 54.8859 mL |
| 5 mM | 0.4391 mL | 2.1954 mL | 4.3909 mL | 10.9772 mL | |
| 10 mM | 0.2195 mL | 1.0977 mL | 2.1954 mL | 5.4886 mL | |
| 15 mM | 0.1464 mL | 0.7318 mL | 1.4636 mL | 3.6591 mL | |
| 20 mM | 0.1098 mL | 0.5489 mL | 1.0977 mL | 2.7443 mL | |
| 25 mM | 0.0878 mL | 0.4391 mL | 0.8782 mL | 2.1954 mL | |
| 30 mM | 0.0732 mL | 0.3659 mL | 0.7318 mL | 1.8295 mL | |
| 40 mM | 0.0549 mL | 0.2744 mL | 0.5489 mL | 1.3721 mL | |
| 50 mM | 0.0439 mL | 0.2195 mL | 0.4391 mL | 1.0977 mL | |
| 60 mM | 0.0366 mL | 0.1830 mL | 0.3659 mL | 0.9148 mL | |
| 80 mM | 0.0274 mL | 0.1372 mL | 0.2744 mL | 0.6861 mL | |
| 100 mM | 0.0220 mL | 0.1098 mL | 0.2195 mL | 0.5489 mL |
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