An inhibitor of PI3Kδ
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Leniolisib

Item No. 28078

Product Insert (PDF)Safety Data Sheet (SDS) (PDF)
Technical Information
Formal Name
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
CAS Number
1354690-24-6
Synonyms
  • CDZ 173
Molecular Formula
C21H25F3N6O2
Formula Weight
450.5
Purity
≥98% (mixture of rotamers)
Formulation (Request formulation change)
A crystalline solid
Solubility(Learn about Variance in Solubility)
DMF: 30 mg/mlDMF:PBS (pH 7.2) (1:1): 0.5 mg/mlDMSO: 25 mg/mlEthanol: 20 mg/ml
λmax
248 nm
SMILES
COC1=NC=C(N2CC(C(N[C@H]3CCN(C(CC)=O)C3)=NC=N4)=C4CC2)C=C1C(F)(F)F
InChi Code
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
InChi Key
MWKYMZXCGYXLPL-ZDUSSCGKSA-N
Shipping & Storage Information
Storage
-20°C
Shipping
Wet ice in continental US; may vary elsewhere
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    1 mg

    $54

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    5 mg

    $250

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    10 mg

    $444

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    25 mg

    $847

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    Product Description

    Leniolisib is an inhibitor of PI3Kδ (IC50 = 0.011 µM).1 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.

    WARNING This product is not for human or veterinary use.

    References & Product Citations
    Product Description References

    1. Hoegenauer, K., Soldermann, N., Zécri, F., et al. Discovery of CDZ173 (leniolisib), representing a structurally novel class of PI3K delta-selective inhibitors. ACS Med. Chem. Lett. 8(9), 975-980 (2017).