Products for Research Use Only

Leniolisib

CAT: 0013-GTR19163763-01Size: 200 mgDry Ice: NoHazardous: No
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CAT#:0013-GTR19163763-01Size:200 mg
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Description
A novel potent and selective PI3Kδ inhibitor with biochemical IC50 of 11 nM; displays >20-fold, 40-fold, and 200-fold selectivity over PI3Kα, PI3Kβ, and PI3Kγ, respectively; shows 30-fold cellular selectivity over PI3Kα; inhibits a large spectrum of immune cell functions, as demonstrated in B and T cells, neutrophils, monocytes, basophils, plasmocytoid dendritic cells, and mast cells in vitro; potently inhibits antigen-specific antibody production and reduces disease symptoms in a rat collagen-induced arthritis model.Other Indication Phase 2 Clinical (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. (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.
CAS Number
1354690-24-6
Product Name Alternative
CDZ-173 | CDZ173
Purity
>98% (HPLC)
Solubility
DMSO: ≥150 mg/mL
Smiles
CCC (=O) N1CCC (C1) NC2=NC=NC3=C2CN (CC3) C4=CC (=C (N=C4) OC) C (F) (F) F
Molecular Formula
C21H25F3N6O2
Molecular Weight
450.4574
Storage Conditions
Storage temperature: -20°C. Stability: ≥ 2 years
Notes
For research use only.
Other Product Names
1-Propanone, 1-[ (3S) -3-[[5,6,7,8-tetrahydro-6-[6-methoxy-5- (trifluoromethyl) -3-pyridinyl]pyrido[4,3-d]pyrimidin-4-yl]amino]-1-pyrrolidinyl]-