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BLU-667 (Pralsetinib)
Pralsetinib (BLU-667) is a clinical-stage, highly potent and selective next generation inhibitor of oncogenic RET fusion and activating mutation with IC50s in low nMs for Wt RET, RET mutants V804L, V804M, M918T and CCDC6-RET fusion, displaying broad and robust anti-tumor activity against multiple RET-driven solid tumor types. It is highly active against V804 gatekeeper substitutions that are mKI resistant. In vivo, BLU-667 potently inhibits growth of NSCLC and thyroid cancer xenografts driven by various RET mutations and fusions without inhibiting VEGFR2. In first-in-human testing, BLU-667 significantly inhibited RET signaling and induced durable clinical responses in patients with RET-altered NSCLC and MTC without notable off-target toxicity.
Catalog NO: CT-BLU667
Synonym: Pralsetinib, BLU667
CAS NO: 2097132-94-8
Mol. Formula: C27H32FN9O2
MW: 533.6 (or, refer to Certificate of Analysis, batch-specific)
** in vivo Quality Material, 99.4-100% pure by achiral and chiral HPLCs, white powder (pic attached), a stereomerically pure single isomer (validated by chiral HPLC), with a spot-on quantitative microanalysis. Bulk stock! Prompt.