Leniolisib

Modify Date: 2025-08-22 13:56:00

Leniolisib Structure
Leniolisib structure
Common Name Leniolisib
CAS Number 1354690-24-6 Molecular Weight 450.45700
Density N/A Boiling Point N/A
Molecular Formula C21H25F3N6O2 Melting Point N/A
MSDS N/A Flash Point N/A

 Use of Leniolisib


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

 Names

Name 1-{(S)-3-[6-(6-methoxy-5-trifluoromethyl-pyridin-3-yl)-5,6,7,8-tetrahydro-pyrido[4,3-d]pyrimidin-4-ylamino]-pyrrolidin-1-yl}-propan-1-one
Synonym More Synonyms

 Leniolisib Biological Activity

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

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].
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

 Chemical & Physical Properties

Molecular Formula C21H25F3N6O2
Molecular Weight 450.45700
Exact Mass 450.19900
PSA 83.48000
LogP 2.96040
Storage condition -20℃

 Synonyms

1-{(S)-3-[6-(6-methoxy-5-trifluoromethyl-pyridin-3-yl)-5,6,7,8-tetrahydro-pyrido[4,3-d]pyrimidin-4-ylamino]-pyrrolidin-1-yl}propan-1-one
(S)-1-(3-(6-(6-Methoxy-5-(trifluoromethyl)pyridin-3-yl)-5,6,7,8-tetrahydropyrido[4,3-d]pyrimidin-4-ylamino)pyrrolidin-1-yl)propan-1-one
{(S)-3-[6-(6-methoxy-5-trifluoromethyl-pyridin-3-yl)-5,6,7,8-tetrahydro-pyrido[4,3-d]pyrimidin-4-ylamino]-pyrrolidin-1-yl}-propan-1-one
Leniolisib
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