Leniolisib

Leniolisib is an inhibitor of PI3Kdelta (IC50 = 0.011 µM). It is selective for PI3Kdelta over PI3Kalpha, PI3Kbeta, and PI3Kgamma (IC50s = 0.244, 0.424, and 2.23 µM, respectively). It inhibits phosphorylation of the PI3K target Akt in Rat-1 fibroblasts expressing P13K p110delta 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 PI3Kdelta-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.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: DMF: 30 mg/ml, DMF:PBS (pH 7.2) (1:1): 0.5 mg/ml, DMSO: 25 mg/ml, Ethanol: 20 mg/ml. lambdamax: 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.