Leniolisib - CAS 1354690-24-6
Catalog number: 1354690-24-6
Category: Inhibitor
Please be kindly noted products are not for therapeutic use. We do not sell to patients.
Molecular Formula:
C21H25F3N6O2
Molecular Weight:
450.46
COA:
Inquire
Targets:
PI3K
Description:
Leniolisib is a PI3K (phosphatidylinositol 3-kinase) inhibitor. No detailed information has been published yet.
Purity:
98%
Appearance:
Powder
Synonyms:
(S)-1-(3-((6-(6-methoxy-5-(trifluoromethyl)pyridin-3-yl)-5,6,7,8-tetrahydropyrido[4,3-d]pyrimidin-4-yl)amino)pyrrolidin-1-yl)propan-1-one;UNII-L22772Z9CP
Solubility:
Soluble in DMSO
Storage:
-20°C Freezer
MSDS:
Inquire
Quality Standard:
In-house standard
Shelf Life:
2 month in rt, long time
Quantity:
Milligrams-Grams
InChIKey:
MWKYMZXCGYXLPL-ZDUSSCGKSA-N
InChI:
1S/C21H25F3N6O2/c1-3-18(31)30-6-4-13(10-30)28-19-15-11-29(7-5-17(15)26-12-27-19)14-8-16(21(22,23)24)20(32-2)25-9-14/h8-9,12-13H,3-7,10-11H2,1-2H3,(H,26,27,28)/t13-/m0/s1
Canonical SMILES:
CCC(=O)N1CC[C@@H](C1)Nc2ncnc3CCN(Cc23)c4cnc(OC)c(c4)C(F)(F)F
1.Discovery of CDZ173 (Leniolisib), Representing a Structurally Novel Class of PI3K Delta-Selective Inhibitors.
Hoegenauer K;Soldermann N;Zécri F;Strang RS;Graveleau N;Wolf RM;Cooke NG;Smith AB;Hollingworth GJ;Blanz J;Gutmann S;Rummel G;Littlewood-Evans A;Burkhart C ACS Med Chem Lett. 2017 Aug 25;8(9):975-980. doi: 10.1021/acsmedchemlett.7b00293. eCollection 2017 Sep 14.
The predominant expression of phosphoinositide 3-kinase δ (PI3Kδ) in leukocytes and its critical role in B and T cell functions led to the hypothesis that selective inhibitors of this isoform would have potential as therapeutics for the treatment of allergic and inflammatory disease. Targeting specifically PI3Kδ should avoid potential side effects associated with the ubiquitously expressed PI3Kα and β isoforms. We disclose how morphing the heterocyclic core of previously discovered 4,6-diaryl quinazolines to a significantly less lipophilic 5,6,7,8-tetrahydropyrido[4,3-;d;]pyrimidine, followed by replacement of one of the phenyl groups with a pyrrolidine-3-amine, led to a compound series with an optimal on-target profile and good ADME properties. A final lipophilicity adjustment led to the discovery of CDZ173 (leniolisib), a potent PI3Kδ selective inhibitor with suitable properties and efficacy for clinical development as an anti-inflammatory therapeutic. ;In vitro;, CDZ173 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 vivo;, CDZ173 inhibits B cell activation in rats and monkeys in a concentration- and time-dependent manner.
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