ONC212

ONC212 is an agonist of the orphan G protein-coupled receptor GPR132 (EC50 = ~400 nM in a PathHunter(R) beta-arrestin assay). It inhibits cell growth in a panel of 62 human leukemia cell lines, including acute myeloid leukemia (AML), acute lymphoblastic leukemia (ALL), chronic myelogenous leukemia (CML), and hairy cell leukemias, with GI50 values ranging from less than 78 to 456 nM. ONC212 also reduces cell growth in a panel of 58 lymphoma cell lines (GI50s = In vivo, ONC212 (50 mg/kg) reduces tumor volume in HT-29 and HCT116 mouse xenograft models.Formal Name: 2,4,6,7,8,9-hexahydro-7-(phenylmethyl)-4-[[4-(trifluoromethyl)phenyl]methyl]-imidazo[1,2-a]pyrido[3,4-e]pyrimidin-5(1H)-one. CAS Number: 1807861-48-8. Molecular Formula: C24H23F3N4O. Formula Weight: 440.5. Purity: >98%. Formulation: (Request formulation change), A crystalline solid. Solubility: DMF: 1 mg/ml, DMSO: 1 mg/ml, DMSO:PBS (pH 7.2) (1:3): 0.25 mg/ml. lambdamax: 232 nm. SMILES: O=C(N(CC1=CC=C(C(F)(F)F)C=C1)C2=NCCN23)C4=C3CCN(C4)CC5=CC=CC=C5. InChi Code: InChI=1S/C24H23F3N4O/c25-24(26,27)19-8-6-18(7-9-19)15-31-22(32)20-16-29(14-17-4-2-1-3-5-17)12-10-21(20)30-13-11-28-23(30)31/h1-9H,10-16H2. InChi Key: DFULPGUTXZTYKA-UHFFFAOYSA-N.