Leniolisib

本公司产品仅用于科研实验，不得用于人体或动物的临床与诊断

一种新型强效选择性 PI3Kδ 抑制剂，生化 IC50 为 11 nM；分别比 PI3Kα、PI3Kβ 和 PI3Kγ 显示 >20 倍、40 倍和 200 倍的选择性。

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.

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.

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.

CDZ-173 | CDZ173

PI3K/Akt/mTOR signaling

PI3K

PI3Kδ|PI3Kα|PI3Kβ|DNA-PK

Other Indications

Other Disease

1354690-24-6

450.4574

C21H25F3N6O2

>98% (HPLC)

DMSO: ≥150 mg/mL

CCC(=O)N1CCC(C1)NC2=NC=NC3=C2CN(CC3)C4=CC(=C(N=C4)OC)C(F)(F)F

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]-

(-20℃)

With Ice Pack

≥ 2 years