prn1371

PRN1371 is an orally available small molecule that acts as a highly specific irreversible covalent inhibitor of fibroblast growth factor receptor types 1–4 (FGFR1–4). It binds to a conserved cysteine residue in the glycine-rich loop of FGFRs and inhibits their tyrosine kinase activity. This inhibition blocks downstream signaling pathways involved in tumor cell proliferation and angiogenesis and can induce tumor cell death. PRN1371 has demonstrated strong potency against FGFR-aberrant cancer cell lines with high selectivity over other kinases. It was developed for the treatment of various cancers harboring genetic alterations in the FGF signaling pathway but clinical development was suspended after phase I trials for solid tumors and urogenital cancers. The drug was originally developed by Principia Biopharma and later acquired by Sanofi[1][2][4][7].

Other names

1802929-43-68-(3-(4-acryloylpiperazin-1-yl)propyl)-6-(2,6-dichloro-3,5-dimethoxyphenyl)-2-(methylamino)pyrido[2,3-d]pyrimidin-7(8H)-one6-(2,6-dichloro-3,5-dimethoxyphenyl)-2-(methylamino)-8-[3-(4-prop-2-enoylpiperazin-1-yl)propyl]pyrido[2,3-d]pyrimidin-7-one