Leniolisib

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Leniolisib

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Cat No: 28078

Biochemicals - Kinase Inhibitors

Leniolisib is an inhibitor of PI3Kδ (IC50 = 0.011 µM).{40219} It is selective for PI3Kδ over PI3Kα, PI3Kβ, and PI3Kγ (IC50s = 0.244, 0.424, and 2.23 µM, respectively). It inhibits phosphorylation of the PI3K target Akt in Rat-1 fibroblasts expressing ...

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Territorial Availability: Available through Bertin Technologies only in France

Synonyms:

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]-1-propanone

Correlated keywords:

1654748-57-8 PI3K ? ? ? PI3 K? K? K? Rat1 p 110? CIA CDZ173

Product Overview:
Leniolisib is an inhibitor of PI3Kδ (IC50 = 0.011 µM).{40219} It is selective for PI3Kδ over PI3Kα, PI3Kβ, and PI3Kγ (IC50s = 0.244, 0.424, and 2.23 µM, respectively). It inhibits phosphorylation of the PI3K target Akt in Rat-1 fibroblasts expressing P13K p110δ with an IC50 value of 0.056 µM. Leniolisib inhibits the mixed lymphocyte reaction (MLR), indicating inhibition of allogeneic T cell activation, in isolated human peripheral blood mononuclear cells (PBMCs) and isolated mouse splenocytes (IC50s = 0.079 and 0.033 µM, respectively). It also inhibits PI3Kδ-dependent B cell activation and IgM-induced B cell proliferation in isolated mouse splenocytes. Leniolisib (3 and 10 mg/kg) reduces the production of rat anti-rat collagen antibodies, as well as reduces paw swelling and joint erosion in a rat model of collagen-induced arthritis.

Size	1 mg
Shipping	dry ice
CAS Number	1354690-24-6
Molecular Formula	C₂₁H₂₅F₃N₆O₂
SMILES	COC1=NC=C(N2CC(C(N[C@H]3CCN(C(CC)=O)C3)=NC=N4)=C4CC2)C=C1C(F)(F)F
Molecular Weight	450,5
Formulation	A crystalline solid
Purity	≥98% (mixture of rotamers)
Custom Code	2933.39
UNSPSC code	12352100

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Cayman Chemical's mission is to help make research possible by supplying scientists worldwide with the basic research tools necessary for advancing human and animal health. Our utmost commitment to healthcare researchers is to offer the highest quality products with an affordable pricing policy.

Our scientists are experts in the synthesis, purification, and characterization of biochemicals ranging from small drug-like heterocycles to complex biolipids, fatty acids, and many others. We are also highly skilled in all aspects of assay and antibody development, protein expression, crystallization, and structure determination.

Over the past thirty years, Cayman developed a deep knowledge base in lipid biochemistry, including research involving the arachidonic acid cascade, inositol phosphates, and cannabinoids. This knowledge enabled the production of reagents of exceptional quality for cancer, oxidative injury, epigenetics, neuroscience, inflammation, metabolism, and many additional lines of research.

Our organic and analytical chemists specialize in the rapid development of manufacturing processes and analytical methods to carry out clinical and commercial GMP-API production. Pre-clinical drug discovery efforts are currently underway in the areas of bone restoration and repair, muscular dystrophy, oncology, and inflammation. A separate group of Ph.D.-level scientists are dedicated to offering Hit-to-Lead Discovery and Profiling Services for epigenetic targets. Our knowledgeable chemists can be contracted to perform complete sample analysis for analytes measured by the majority of our assays. We also offer a wide range of analytical services using LC-MS/MS, HPLC, GC, and many other techniques.

Accreditations
ISO/IEC 17025:2005
ISO Guide 34:2009

Cayman is a leader in the field of emerging drugs of abuse, providing high-purity Schedule I-V Controlled Substances to federally-licensed laboratories and qualified academic research institutions for forensic analyses. We are certified by ACLASS Accreditation Services with dual accreditation to ISO/IEC 17025:2005 and ISO Guide 34:2009.