Bimiralisib

Bimiralisib is a potent and orally bioavailable inhibitor of phosphatidylinositol 3-kinases (PI3Ks, IC50s = 33, 661, 708, and 451 nM for PI3Kalpha, PI3Kbeta, PI3Kgamma, and PI3Kdelta, respectively) and the mammalian target of rapamycin (mTOR, IC50 = 89 nM). It is selective for these kinases over a panel of cell surface and nuclear receptors, membrane channels, transporters, kinases, proteases, and phosphodiesterases at a concentration of 10 µM. Bimiralisib has anticancer activity with an average GI50 value of 0.7 µM across the National Cancer Institute (NCI) 60 human cancer cell line panel. In vivo, bimiralisib (5-15 mg/kg) reduces tumor growth in a dose-dependent manner in a PC3 prostate cancer mouse xenograft model. Formulations containing bimiralisib are under clinical investigation for the treatment of relapsed and refractory lymphoma and advanced solid tumors.Formal Name: 5-(4,6-di-4-morpholinyl-1,3,5-triazin-2-yl)-4-(trifluoromethyl)-2-pyridinamine. CAS Number: 1225037-39-7. Synonyms: PI3K-IN-2. Molecular Formula: C17H20F3N7O2. Formula Weight: 411.4. Purity: >98%. Formulation: (Request formulation change), A crystalline solid. Solubility: DMF: 10 mg/ml, DMSO: 10 mg/ml, Ethanol: 2 mg/ml. lambdamax: 203, 233, 279 nm. SMILES: NC(N=C1)=CC(C(F)(F)F)=C1C2=NC(N3CCOCC3)=NC(N4CCOCC4)=N2. InChi Code: InChI=1S/C17H20F3N7O2/c18-17(19,20)12-9-13(21)22-10-11(12)14-23-15(26-1-5-28-6-2-26)25-16(24-14)27-3-7-29-8-4-27/h9-10H,1-8H2,(H2,21,22). InChi Key: ADGGYDAFIHSYFI-UHFFFAOYSA-N.