Description
Information(R)-GNE-140 (R)-GNE-140 is a selective inhibitor of the LDHA and LDHB with IC50s of 3 nM and 5 nM, respectively. The R enantiomer of GNE-140 is 18-fold more potent than S enantiomer.TargetsLDHA (Cell-free assay); LDHB (Cell-free assay) 3 nM; 5 nMIn vitro(R)-GNE-140 inhibits proliferation in 37 of 347 cancer cell lines tested at a potency cut off of 5 µM. (R)-GNE-140 exhibits inhibition with two chondrosarcoma (bone) cancer cell lines that harbored IDH1 mutations (IC50 = 0.8µM).(R)-GNE-140 has submicromolar MiaPaca2 potency and inhibits proliferation in 11% of cancer cell lines in a broad panel.In vivo(R)-GNE-140 presents a low Clp, and also had high bioavailability when dosed orally at 5 mg/kg to mice. At higher oral doses, ranging from 50 to 200 mg/kg, (R)-GNE-140 displays greater in vivo exposure.Cell Research(from reference)Cell lines：105KC,JJ012,143B,G84,1321N1,ONS-76,G22,G140,G96,HCC1143,CAL-120,Hs 578T,SISO,SKG-II,HCT-15,KYSE-520,KMRC-1,SNU-475,SNU-423,HT-1080,NCI-H1437,NCI-H1339,LXF-289,MCAS,PA-1,Hs 38.T,59M,MIA PaCa-2,SW 1990,PSN1,GR-M,Hs 746T,MKN-74,S-117,FTC-238,B-CP Concentrations：6 pt dose titration scheme Incubation Time：72 h