Leniolisib structure
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Common Name | Leniolisib | ||
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| 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 LeniolisibLeniolisib (CDZ173) is a potent and selective PI3Kδ inhibitor currently in phase II/III clinical trials for the treatment of immunodeficiency disorders. |
| 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 |
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| Synonym | More Synonyms |
| Description | Leniolisib (CDZ173) is a potent and selective PI3Kδ inhibitor currently in phase II/III clinical trials for the treatment of immunodeficiency disorders. |
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| 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 |
| Molecular Formula | C21H25F3N6O2 |
|---|---|
| Molecular Weight | 450.45700 |
| Exact Mass | 450.19900 |
| PSA | 83.48000 |
| LogP | 2.96040 |
| Storage condition | -20℃ |
| 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 |