Pralsetinib (BLU-667) (C09-1017-283)

InformationPralsetinib (BLU-667) Pralsetinib (BLU-667, CS 3009, Gavreto) is a highly potent and selective RET (c-RET) inhibitor with an IC50 of 0.4 nM for WT RET. It also demonstrates potent activity (IC50 0.4 nmol/L) against common oncogenic RET alterations, including RET (M918T).TargetsRET V804L (Cell-free assay ); WT RET (Cell-free assay); RET V804M (Cell-free assay); RET M918T (Cell-free asssay); CCDC6-RET (Cell-free assay) 31895,0.3 nM; 0.4 nM; 0.4 nM; 0.4 nM; 0.4 nMIn vitroBLU-667 is at least 100-fold more selective for RET over 96% of kinases tested (a panel of 371 kinases). BLU-667 specifically abrogates RET signaling in RET-altered cancers from diverse lineages. RET pathway inhibition with BLU-667 also more potently inhibits proliferation of RET-altered cell lines relative to multikinase inhibitors.In vivoBLU-667 potently inhibits growth of NSCLC and thyroid cancer xenografts driven by various RET mutations and fusions without inhibiting VEGFR2. BLU-667 is well tolerated throughout the in vivo studies.Cell Research(from reference)Cell lines：LC2/ad cells,/u3000MZ-CRC-1 cells and TT cells Concentrations：0-1 μM Incubation Time：90 minutes. Specification: 0.98 Molecular Formula: C27H32FN9O2 Molecular Weight: 533.6 PubChem CID: 129073603 Isomeric SMILES: CC1=CC(=NN1)NC2=NC(=NC(=C2)C)C3CCC(CC3)(C(=O)N[C@@H](C)C4=CN=C(C=C4)N5C=C(C=N5)F)OC