Leniolisib (Synonyms: CDZ 173) |
رقم الكتالوجGC19471
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Leniolisib (CDZ173) هو مثبط قوي وانتقائي PI3Kδ
Products are for research use only. Not for human use. We do not sell to patients.
Cas No.: 1354690-24-6
Sample solution is provided at 25 µL, 10mM.
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Leniolisib (CDZ173) is a potent and selective PI3Kδ inhibitor currently in phase II/III clinical trials for the treatment of immunodeficiency disorders.
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].
Oral leniolisib lead to a dose-dependent reduction in PI3K/AKT pathway activity and resolve the immune dysregulation with normalization of circulating transitional and naïve B cells and reduction in PD-1+CD4+ and senescent CD57+CD8+ T cells. After 12 weeks of treatment, all patients show amelioration of lymphoproliferation with lymph node sizes and spleen volumes reduced by 39% (mean, range 26-57%) and 40% (mean, range: 13-65%), respectively[1].
Reference:
[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
| Cas No. | 1354690-24-6 | SDF | |
| المرادفات | CDZ 173 | ||
| Canonical SMILES | CCC(N1C[C@@H](NC2=C(CN(C3=CC(C(F)(F)F)=C(OC)N=C3)CC4)C4=NC=N2)CC1)=O | ||
| Formula | C₂₁H₂₅F₃N₆O₂ | M.Wt | 450.46 |
| الذوبان | DMF: 30 mg/ml,DMF:PBS (pH 7.2) (1:1): 0.5 mg/ml,DMSO: 25 mg/ml,Ethanol: 20 mg/ml | Storage | Store at -20°C |
| General tips | Please select the appropriate solvent to prepare the stock solution according to the
solubility of the product in different solvents; once the solution is prepared, please store it in
separate packages to avoid product failure caused by repeated freezing and thawing.Storage method
and period of the stock solution: When stored at -80°C, please use it within 6 months; when stored
at -20°C, please use it within 1 month. To increase solubility, heat the tube to 37°C and then oscillate in an ultrasonic bath for some time. |
||
| Shipping Condition | Evaluation sample solution: shipped with blue ice. All other sizes available: with RT, or with Blue Ice upon request. | ||
| Prepare stock solution | |||
|
1 mg | 5 mg | 10 mg |
| 1 mM | 2.22 mL | 11.0998 mL | 22.1995 mL |
| 5 mM | 444 μL | 2.22 mL | 4.4399 mL |
| 10 mM | 222 μL | 1.11 mL | 2.22 mL |
Step 1: Enter information below (Recommended: An additional animal making an allowance for loss during the experiment)
g
μL
Step 2: Enter the in vivo formulation (This is only the calculator, not formulation. Please contact us first if there is no in vivo formulation at the solubility Section.)
Calculation results:
Working concentration: mg/ml;
Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid concentration mg/mL, Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug. )
Method for preparing in vivo formulation: Take μL DMSO master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL saline, mix and clarify.
Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.
Note: 1. Please make sure the liquid is clear before adding the next solvent.
2. Be sure to add the solvent(s) in order. You must ensure that the solution obtained, in the previous addition, is a clear solution before proceeding to add the next solvent. Physical methods such as vortex, ultrasound or hot water bath can be used to aid dissolving.
3. All of the above co-solvents are available for purchase on the GlpBio website.
Quality Control & SDS
- View current batch:
- Purity: >99.00% Appearance: A solid
- COA (Certificate of Analysis)
- SDS (Safety Data Sheet)
- Datasheet
Average Rating: 5 (Based on Reviews and 36 reference(s) in Google Scholar.)