cis-pralsetinib

trans-Pralsetinib (trans-BLU-667) is a potent inhibitor of the RET (Rearranged during Transfection) kinase. This compound originates from Compound Example 129 in patent US20170121312A1. RET is a receptor tyrosine kinase whose genetic rearrangements or mutations are key drivers in various cancers, including non-small cell lung cancer (NSCLC) and medullary thyroid cancer. By inhibiting RET kinase activity, trans-Pralsetinib blocks downstream oncogenic signaling pathways, thereby exerting anti-tumor effects.

Pralsetinib (Blu667) (BLU-667) is a highly potent, selective RET inhibitor (IC50s: 0.4, 0.3, 0.4, 0.4, and 0.4 nM for WT RET, RET mutants V804L, V804M, M918T and CCDC6-RET fusion).

Pralsetinib is a selective and next-generation RET inhibitor (IC50: 0.3-0.4 nM for WT RET, RET mutants V804L, V804M, M918T, and CCDC6-RET fusion). BLU-667 is an effective and selective inhibitor of RET mutations, fusions, and predicted resistant mutants.