BLU-667 (PRALSETINIB) (BLU667)

Description

Background Information:

BLU-667 (Pralsetinib) 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.

Reference:

1. V. Subbiah, et al, Precision Targeted Therapy With BLU-667 for RET-Driven Cancers, Cancer Discovery, 2018 Jul; 8(7):836-849. doi: 10.1158/2159-8290.CD-18-0338.

APIM050116: BLU-667 (PRALSETINIB) (BLU667)

CAS No.: 2097132-94-8.
Molecular Formula: C27H32FN9O2.
Molecular Weight: 533.6 (or, refer to Certificate of Analysis, batch-specific).
Purity: >99% chemical and optical purity by achiral and chiral HPLCs.
QC: Achiral and Chiral HPLCs, MS, 1H-NMR, and Quantitative Elemental Analysis Report.
Solubility: Refer to Certificate of Analysis.
Storage: Refer to Certificate of Analysis.

Additional information

Ship from Country	USA
Size	10 mg, 5 mg, 50 mg

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