Cat. No.: HY-17635

Leniolisib

(Synonyms: CDZ173)

1 Cited Publications

Customer Review

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.

For research use only. We do not sell to patients.

Purity: 99.38%
CAS No.: 1354690-24-6
Formula: C₂₁H₂₅F₃N₆O₂
Molecular Weight:450.46

Storage:

Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 2 years , -20°C, 1 year

Leniolisib Chemical Structure

CAS No.: 1354690-24-6

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Fluorescent Dye

Strong Fluorescence Signal / Multi-Disciplinary Applications / High Fluorescence Specificity

Biological Activity
- Description
- IC₅₀ & Target
- Cellular Effect
- In Vitro
- In Vivo
- Clinical Trial
Chemical Information
Publications (1)
Solvent & Solubility
- In Vitro
- In Vivo
Purity & Documentation
References
Help & FAQs
Bioz

Biological Activity

Description

Leniolisib (CDZ173) is a potent and selective PI3Kδ inhibitor. Leniolisib has the potential for immunodeficiency disorders treatment.

IC₅₀ & Target^[1]

PI3Kδ

11 nM (IC₅₀)

PI3Kα

280 nM (IC₅₀)

PI3Kβ

480 nM (IC₅₀)

PI3Kγ

2.57 μM (IC₅₀)

DNA-PK

880 nM (IC₅₀)

All PI3K Isoforms :

Cellular Effect

Cell Line	Type	Value	Description	References
DOHH-2	IC₅₀	29.2 μM Compound: Fig 1, Cpd 9; CDZ173	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	[PMID: 35609190]
JeKo-1	IC₅₀	31.66 μM Compound: Fig 1, Cpd 9; CDZ173	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	[PMID: 35609190]
Pfeiffer	IC₅₀	3.75 μM Compound: Fig 1, Cpd 9; CDZ173	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	[PMID: 35609190]
Rec1	IC₅₀	1.28 μM Compound: Fig 1, Cpd 9; CDZ173	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	[PMID: 35609190]
SUD4	IC₅₀	8.25 μM Compound: Fig 1, Cpd 9; CDZ173	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	[PMID: 35609190]
SU-DHL-6	IC₅₀	0.77 μM Compound: Fig 1, Cpd 9; CDZ173	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	[PMID: 35609190]
Z-138	IC₅₀	31.19 μM Compound: Fig 1, Cpd 9; CDZ173	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	[PMID: 35609190]

In Vitro

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.

In Vivo

Oral leniolisib lead to a dose-dependent reduction in PI3K/AKT pathway activity and resolve the immune dysregulation with normalization of circulating transitional and na ve 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].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Clinical Trial

NCT Number	Sponsor	Condition	Start Date	Phase A549
NCT01329991	Plexxikon\|		2011-05	PHASE1

Chemical Information

CAS No. 1354690-24-6
Appearance Solid
Molecular Weight 450.46
Formula C₂₁H₂₅F₃N₆O₂
Color White to off-white
SMILES

CCC(N1C[C@@H](NC2=C(CN(C3=CC(C(F)(F)F)=C(OC)N=C3)CC4)C4=NC=N2)CC1)=O
Synonyms

CDZ173
Shipping

Room temperature in continental US; may vary elsewhere.

Storage

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

Mol Syst Biol

Illuminating phenotypic drug responses of sarcoma cells to kinase inhibitors by phosphoproteomics. [Abstract]

2024 Jan;20(1):28-55. PMID: 38177929

Solvent & Solubility

In Vitro:

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)

View the Complete Stock Solution Preparation Table

Preparing Stock Solutions

View the Complete Stock Solution Preparation Table

Concentration Solvent Mass

1 mg

5 mg

10 mg

Concentration

Solvent

Mass

1 mM

2.2200 mL

11.0998 mL

22.1995 mL

5 mM

0.4440 mL

2.2200 mL

4.4399 mL

10 mM

0.2220 mL

1.1100 mL

2.2200 mL

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.

Molarity Calculator

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

Mass Mass

Concentration Concentration

Volume Volume

Molecular Weight Molecular Weight

Dilution Calculator

Concentration _(start) × Volume _(start) = Concentration _(final) × Volume _(final)

Concentration _(start) Concentration _(start)

Volume _(start) Volume _(start)

Concentration _(final) Concentration _(final)

Volume _(final) Volume _(final)

In Vivo:

Select the appropriate dissolution method based on your experimental animal and administration route.

Stock Solution Working Solution

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.

Protocol 1

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.

Protocol 2

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.

Protocol 3

Add each solvent one by one: 10% DMSO 90% Corn Oil

Solubility: ≥ 2.5 mg/mL (5.55 mM); Clear solution

This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown). If the continuous dosing period exceeds half a month, please choose this protocol carefully.

Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 900 μL Corn oil, and mix evenly.

In Vivo Dissolution Calculator

Please enter the basic information of animal experiments:

Dosage Dosage
mg/kg
Animal Weight (Per Animal) Animal Weight (Per Animal)
g
Dosing Volume (Per Animal) Dosing Volume (Per Animal)
μL
Number of Animals Number of Animals

Recommended: Prepare an additional quantity of animals to account for potential losses during 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

Purity & Documentation

Select Batch:

Purity: 99.98%

Assay: 99.98%

ee.: 99.98%

Data Sheet (280 KB)
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)
COA (2659 KB)
Elemental Analysis Report (2659 KB)
HNMR (2659 KB)
CNMR (2659 KB)
RP-HPLC (2659 KB)
NP-HPLC (2659 KB)
MS (2659 KB)
LCMS (2659 KB)
IR (2659 KB)
GC (2659 KB)
OR (2659 KB)
SDS-PAGE (2659 KB)
SEC-HPLC (2659 KB)
Other Report (2659 KB)
Handling Instructions (2659 KB)

References

[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]

Help & FAQs

How should lyophilized recombinant proteins be reconstituted and stored?

1. Before opening the cap, centrifuge the vial at 13000 rpm for 20-30 seconds. This step will ensure that any lyophilized powder that may have adhered to the cap or walls is collected at the bottom of the vial, minimizing the risk of product loss.

Complete Stock Solution Preparation Table

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

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Leniolisib

Immunology/Inflammation Compound Library

Kinase Inhibitor Library

PI3K/Akt/mTOR Compound Library

Stem Cell Signaling Compound Library

FDA-Approved Drug Library

Autophagy Compound Library

Anti-Aging Compound Library

Drug Repurposing Compound Library

Differentiation Inducing Compound Library

Oxygen Sensing Compound Library

Glycolysis Compound Library

Cytoskeleton Compound Library

FDA Approved & Pharmacopeial Drug Library

Anti-Breast Cancer Compound Library

Anti-Lung Cancer Compound Library

Anti-Pancreatic Cancer Compound Library

Anti-Blood Cancer Compound Library

Anti-Cancer Metabolism Compound Library

Anti-Obesity Compound Library

Angiogenesis-Related Compound Library

Glucose Metabolism Compound Library

Anti-Liver Cancer Compound Library

Rare Diseases Drug Library

Anti-Colorectal Cancer Compound Library

Anti-Prostate Cancer Compound Library

Anti-Pulmonary Fibrosis Compound Library

Cancer Stem Cells Compound Library

Heterocyclic Compound Library

Pain-Related Compound Library

Membrane Protein-targeted Compound Library

Highly Selective Inhibitors Library

Anti-Hematopathy Compound Library

Anti-Ovarian Cancer Compound Library

Multi-Target Compound Library

Bioactive Compound Library Max

MCE Bioactive Compound Library

Drug Repurposing Compound Library Plus

FDA-Approved Drug Library Plus

FDA-Approved Drug Library Mini

Bioactive Compound Library

Anti-Fibrosis Compound Library

Anti-Brain Cancer Compound Library

Cell Proliferation Compound Library

High-Throughput Bioactive Compound Library

Anti-Rheumatic Arthritis Compound Library

Posttranslational Modification Library

FDA Kinase Inhibitor Library

Lactylation Compound Library

Publications Citing Use of MedChemExpress (MCE) Leniolisib

All PI3K Isoforms

Biological Activity

Chemical Information

Publications (1)

Solvent & Solubility

Purity & Documentation

References

Help & FAQs

Complete Stock Solution Preparation Table

Leniolisib Related Classifications

Cat. No.: HY-17635