OPB-171775

OPB-171775 is a molecular glue. It induces the formation of a complex between phosphodiesterase 3A (PDE3A) and ribonuclease SLFN12. OBI-171775 (10 nM) induces G0/G1 phase cell cycle arrest, apoptosis, and necrosis in PFSK-1 primitive neuroectodermal tumor cells, with cell cycle arrest partially blocked by the general control nonderepressible 2 kinase (GCN2) inhibitor GCN2iB (Cay35897). It reduces tumor volume and induces tumor regression in patient-derived xenograft (PDX) mouse models of a variety of cancer types, including gastrointestinal stromal tumor (GIST), ovarian, and lung cancers. OPB-171775 (0.03 mg/kg) reduces tumor growth in a GS11353 PDX mouse model of GIST, with tumor eradication when administered in combination with imatinib (Cay13139).. SMILES: FC1=C(C2=NNC(C[C@H]2C)=O)C=CC(OCC(C)(O)C)=C1F. InChi Code: InChI=1S/C15H18F2N2O3/c1-8-6-11(20)18-19-14(8)9-4-5-10(13(17)12(9)16)22-7-15(2,3)21/h4-5,8,21H,6-7H2,1-3H3,(H,18,20)/t8-/m1/s1. InChi Key: GGUTYKLJESECBW-MRVPVSSYSA-N