Roginolisib

Roginolisib is an inhibitor of PI3Kdelta (IC50 = 0. µM). It is selective for PI3Kdelta over PI3Kalpha, PI3Kbeta, PI3Kgamma, VPS34, and PI3KC2beta (IC50s = 0. 1. 10. 5. and 5. µM, respectively). Roginolisib inhibits the growth of SU-DHL-6 B cell lymphoma cells that endogenously express PI3Kdelta (GI50 = 0. µM) but not cancer cell lines endogenously expressing PI3Kalpha, PI3Kbeta, or PI3Kgamma. In vivo, roginolisib (30 mg/kg twice daily) alone or in combination with an anti-PD-1 antibody slows tumor growth and decreases tumor volume in a murine Lewis lung carcinoma model. Formal Name: [6-fluoro-1,4-dihydro-1-[4-(4-morpholinylmethyl)phenyl]-5,5-dioxido[1]benzothiopyrano[4,3-c]pyrazol-3-yl]-4-morpholinyl-methanone. CAS Number: 1305267-37-1. Synonyms: IOA-244 MSC2360844. Molecular Formula: C26H27FN4O5S. Formula Weight: 526.6. Purity: >98%. Formulation (Request formulation change): A solid. Solubility: Acetonitrile:Water (1:1): Slightly soluble: 0.1-1 mg/ml. SMILES: O=S1(CC2=C(N(C3=CC=C(CN4CCOCC4)C=C3)N=C2C(N5CCOCC5)=O)C6=C1C(F)=CC=C6)=O. InChi Code: InChI=1S/C26H27FN4O5S/c27-22-3-1-2-20-24-21(17-37(33,34)25(20)22)23(26(32)30-10-14-36-15-11-30)28-31(24)19-6-4-18(5-7-19)16-29-8-12-35-13-9-29/h1-7H,8-17H2. InChi Key: NFHSJYKXENYICE-UHFFFAOYSA-N. Storage: -20°C. Stability: > 4 years.