Tenalisib

Tenalisib is an inhibitor of PI3Kdelta and PI3Kgamma (IC50s = 24.5 and 33.2 nM, respectively). It is greater than 300- and 120-fold selective for PI3Kdelta and PI3Kgamma, respectively, over PI3Kalpha and PI3Kbeta. Tenalisib (10 µM) induces cell death in L-540, KM-H2, and L-428 Hodgkin lymphoma cells. It induces cell cycle arrest at the G0/G1 phase in the same cells. In vivo, tenalisib reduces tumor growth and vasculature, induces tumor necrosis, and induces the M1 phenotype in tumor-associated macrophages (TAMs) in an L-540 mouse xenograft model.Formal Name: 3-(3-fluorophenyl)-2-[(1S)-1-(9H-purin-6-ylamino)propyl]-4H-1-benzopyran-4-one. CAS Number: 1639417-53-0. Synonyms: RP 6530. Molecular Formula: C23H18FN5O2. Formula Weight: 415.4. Purity: >98%. Formulation: (Request formulation change), A solid. Solubility: :, DMSO: Soluble: >10 mg/ml, Ethanol: Sparingly soluble: 1-10 mg/ml. SMILES: O=C1C(C2=CC=CC(F)=C2)=C([C@H](CC)NC3=C4C(N=CN4)=NC=N3)OC5=CC=CC=C51. InChi Code: InChI=1S/C23H18FN5O2/c1-2-16(29-23-19-22(26-11-25-19)27-12-28-23)21-18(13-6-5-7-14(24)10-13)20(30)15-8-3-4-9-17(15)31-21/h3-12,16H,2H2,1H3,(H2,25,26,27,28,29)/t16-/m0/s1. InChi Key: HDXDQPRPFRKGKZ-INIZCTEOSA-N.