rg-1530

RG1530 is an orally active small molecule multikinase inhibitor developed for the treatment of advanced solid tumors. It exhibits high affinity for Polo like kinase 4 (PLK4) and inhibits multiple receptor tyrosine kinases involved in angiogenesis such as Vascular endothelial growth factor receptor 1 (VEGFR1), Vascular endothelial growth factor receptor 2 (VEGFR2), Vascular endothelial growth factor receptor 3 (VEGFR3), Platelet-derived growth factor receptor beta (PDGFRB), FMS-like tyrosine kinase 3 (Flt3), and Fibroblast growth factor receptor 1 (FGFR1) and Fibroblast growth factor receptor 2 (FGFR2). The drug acts as a mitosis–angiogenesis inhibitor by inducing mitotic arrest and apoptosis in cancer cells while sparing normal proliferating cells. Preclinical studies demonstrated potent antiproliferative activity against tumor cell lines and significant tumor regression in xenograft models of lung, colorectal, prostate and breast cancers. Clinical development reached phase I trials but was discontinued[1][2][5][7].

Other names

5-(2-chlorophenyl)-7-fluoro-1,2-dihydro-8-methoxy-3-methylpyrazolo[3,4-b][1,4]benzodiazepine5-(2-chlorophenyl)-7-fluoro-8-methoxy-3-methyl-1,2-dihydropyrazolo[3,4-b][1,4]benzodiazepine5-(2-chlorophenyl)-7-fluoro-8-methoxy-3-methylpyrazolo(3,4-b)(1,4)benzodiazepineCHEMBL1980391CHEMBL-1980391CHEMBL 1980391UNII-XQJ55R5PPQUNII-XQJ-55R5PPQUNII-XQJ 55R5PPQ