1. PI3K/Akt/mTOR
  2. PI3K
  3. Leniolisib

Leniolisib (Synonyms: CDZ173)

Cat. No.: HY-17635 Purity: 99.62%
Handling Instructions

Leniolisib (CDZ173) is a potent and selective PI3Kδ inhibitor currently in phase II/III clinical trials for the treatment of immunodeficiency disorders.

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

Leniolisib Chemical Structure

Leniolisib Chemical Structure

CAS No. : 1354690-24-6

Size Price Stock Quantity
10 mM * 1 mL in DMSO USD 208 In-stock
Estimated Time of Arrival: December 31
1 mg USD 90 In-stock
Estimated Time of Arrival: December 31
5 mg USD 210 In-stock
Estimated Time of Arrival: December 31
10 mg USD 350 In-stock
Estimated Time of Arrival: December 31
50 mg USD 1200 In-stock
Estimated Time of Arrival: December 31
100 mg USD 2100 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

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Description

Leniolisib (CDZ173) is a potent and selective PI3Kδ inhibitor currently in phase II/III clinical trials for the treatment of immunodeficiency disorders.

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)

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].

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].

Clinical Trial
Molecular Weight

450.46

Formula

C₂₁H₂₅F₃N₆O₂

CAS No.

1354690-24-6

SMILES

CCC(N1C[[email protected]@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 6 months
  -20°C 1 month
Solvent & Solubility
In Vitro: 

DMSO : 100 mg/mL (222.00 mM; Need ultrasonic)

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
*Please refer to the solubility information to select the appropriate solvent.
In Vivo:
  • 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

  • 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

  • 3.

    Add each solvent one by one:  10% DMSO    90% corn oil

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

*All of the co-solvents are provided by MCE.
References

Purity: 99.62%

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Keywords:

LeniolisibCDZ173CDZ 173CDZ-173PI3KPhosphoinositide 3-kinaseInhibitorinhibitorinhibit

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Product name:
Leniolisib
Cat. No.:
HY-17635
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