LB-100

LB-100 is an inhibitor of protein phosphatase 2A (PP2A) with anticancer activity. It reduces PP2A activity and is cytotoxic to BxPC-3 and PANC-1 cells (IC50s = 0.85 and 3.87 µM, respectively). LB-100 inhibits radiation-induced Rad51 focus formation and homologous recombination repair in PANC-1 and MiaPaCa-2 cells. In vivo, it increases tumor microvessel density and VEGF secretion and decreases tumor volume in a PANC-1 mouse xenograft model when administered at a dose of 2 mg/kg. LB-100 (1.5 mg/kg) enhances radiation-induced reductions in tumor volume in CNE1 and CNE2 radioresistant nasopharyngeal carcinoma mouse xenograft models.Formal Name: (1R,4S)-rel-3-[(4-methyl-1-piperazinyl)carbonyl]-7-oxabicyclo[2.2.1]heptane-2-carboxylic acid. CAS Number: 1632032-53-1. Molecular Formula: C13H20N2O4. Formula Weight: 268.3. Purity: >98%. Formulation: (Request formulation change), A crystalline solid. Solubility: Ethanol: Partially soluble, PBS (pH 7.2): 10 mg/ml. SMILES: CN1CCN(C(C2C(C(O)=O)[C@H]3CC[C@@H]2O3)=O)CC1. InChi Code: InChI=1S/C13H20N2O4/c1-14-4-6-15(7-5-14)12(16)10-8-2-3-9(19-8)11(10)13(17)18/h8-11H,2-7H2,1H3,(H,17,18)/t8-,9+,10?,11?/m0/s1. InChi Key: JUQMLSGOTNKJKI-IZUQBHJASA-N.