Leniolisib (Synonyms: CDZ173)

Name: Leniolisib
Brand: MedChemExpress
SKU: HY-17635
Rating: 4.5 (1 reviews)

Cat. No.: HY-17635 Purity: 99.28%: FAQs
Data Sheet SDS COA Handling Instructions

Molarity Calculator

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.

Leniolisib Chemical Structure

CAS No. : 1354690-24-6

Size	Price	Stock	Quantity
Solid + Solvent (Highly Recommended)
10 mM * 1 mL in DMSO ready for reconstitution	USD 208	In-stock	Estimated Time of Arrival: December 31
Solution
10 mM * 1 mL in DMSO	USD 208	In-stock	Estimated Time of Arrival: December 31
Solid
1 mg	USD 90	In-stock	Estimated Time of Arrival: December 31
5 mg	USD 190	In-stock	Estimated Time of Arrival: December 31
10 mg	USD 285	In-stock	Estimated Time of Arrival: December 31
50 mg	USD 830	In-stock	Estimated Time of Arrival: December 31
100 mg	USD 1200	In-stock	Estimated Time of Arrival: December 31
200 mg		Get quote
500 mg		Get quote

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Customer Review

Based on 1 publication(s) in Google Scholar

Other Forms of Leniolisib:

Leniolisib-d₅ Get quote
Leniolisib phosphate Get quote

1 Publications Citing Use of MCE Leniolisib

•Mol Syst Biol. 2023 Dec 18.

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View All PI3K Isoform Specific Products:

View All Isoforms

PI3Kα PI3Kβ PI3Kγ PI3Kδ PI3KC2α PI3KC2β PI3KC2γ Vps34 PI3K PI3KC3 p120γ

Biological Activity
Purity & Documentation
References
Customer Review

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)

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 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].

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

Clinical Trial

Molecular Weight

450.46

Formula

C₂₁H₂₅F₃N₆O₂

CAS No.

1354690-24-6

Appearance

Solid

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

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

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)

Preparing
Stock Solutions

Concentration Solvent Mass	1 mg	5 mg	10 mg

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

View the 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.

Molarity Calculator
Dilution Calculator

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

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

This equation is commonly abbreviated as: C₁V₁ = C₂V₂

Concentration _(start)

Volume _(start)

Concentration _(final)

Volume _(final)

In Vivo:

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.

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.
Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
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.
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.
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

mg/kg

Animal weight
(per animal)

Dosing volume
(per animal)

μL

Number of animals

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

Please enter your animal formula composition:

DMSO +

Tween-80 +

Saline

Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.

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).

Calculation results:

Working solution concentration: mg/mL

Method for preparing stock solution: mg drug dissolved in μL DMSO (Stock solution concentration: mg/mL).

The concentration of the stock solution you require exceeds the measured solubility. The following solution is for reference only. If necessary, please contact MedChemExpress (MCE).

Method for preparing in vivo working solution for animal experiments: Take μL DMSO stock solution, add μL . μL , mix evenly, next add μL Tween 80, mix evenly, then add μL Saline.

If the continuous dosing period exceeds half a month, please choose this protocol carefully.

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

Purity: 99.28%

Select Batch:

Data Sheet (280 KB) SDS (393 KB)

COA (256 KB) LCMS (95 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]

Complete Stock Solution Preparation Table

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

Inflammation/Immunology

Help & FAQs

Do most proteins show cross-species activity?
Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

Leniolisib1354690-24-6CDZ173CDZ 173CDZ-173PI3KPhosphoinositide 3-kinaseInhibitorinhibitorinhibit

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Leniolisib (Synonyms: CDZ173)

Customer Review

Other Forms of Leniolisib:

Leniolisib Related Antibodies

1 Publications Citing Use of MCE Leniolisib

Featured Recommendations

•Related Screening Libraries:

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View All PI3K Isoform Specific Products:

Biological Activity

Purity & Documentation

References

Customer Review

Leniolisib Related Antibodies

Molarity Calculator

Dilution Calculator

Complete Stock Solution Preparation Table

Leniolisib Related Classifications

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