PQR530

PQR530 is a dual inhibitor of PI3Kalpha and mammalian target of rapamycin (mTOR, IC50s = 11.1 and 7.4 nM, respectively). It inhibits phosphorylation of Akt and ribosomal S6 kinase in A2058 melanoma cells (IC50s = 62.2 and 61.1 nM, respectively). PQR530 inhibits cell growth in a panel of 66 cancer cell lines (mean GI50 = 0.43 µM). In vivo, PQR530 (25 mg/kg) reduces tumor growth in an OVCAR-3 ovarian cancer mouse xenograft model. It decreases the number of seizures per week in a Tsc1GFAP conditional knockout mouse model of epilepsy.Formal Name: 4-(difluoromethyl)-5-[4-[(3S)-3-methyl-4-morpholinyl]-6-(4-morpholinyl)-1,3,5-triazin-2-yl]-2-pyridinamine. CAS Number: 1927857-61-1. Molecular Formula: C18H23F2N7O2. Formula Weight: 407.4. Purity: >98%. Formulation: (Request formulation change), A crystalline solid. Solubility: DMF: 30 mg/ml, DMF:PBS (pH 7.2) (1:3): 0.33 mg/ml, DMSO: 10 mg/ml. lambdamax: 235, 290 nm. SMILES: NC1=NC=C(C2=NC(N3[C@@H](C)COCC3)=NC(N4CCOCC4)=N2)C(C(F)F)=C1. InChi Code: InChI=1S/C18H23F2N7O2/c1-11-10-29-7-4-27(11)18-24-16(13-9-22-14(21)8-12(13)15(19)20)23-17(25-18)26-2-5-28-6-3-26/h8-9,11,15H,2-7,10H2,1H3,(H2,21,22)/t11-/m0/s1. InChi Key: SYKBZXMKAPICSO-NSHDSACASA-N.