Get a Quote

CAS NO.: 2097132-94-8
Chemical Formula: C27H32FN9O2
Molecular Weight: 533.6000
DMF&GMP status: Please contact us for more details.
Pralsetinib is a kinase inhibitor of wild-type RET and oncogenic RET fusions (CCDC6-RET) and mutations (RET V804L, RET V804M and RET M918T) with half maximal inhibitory concentrations (IC50s) less than 0.5 nM. In purified enzyme assays, pralsetinib inhibited DDR1, TRKC, FLT3, JAK1-2, TRKA, VEGFR2, PDGFRb, and FGFR1 at higher concentrations that were still clinically achievable at Cmax. In cellular assays, pralsetinib inhibited RET at approximately 14-, 40-, and 12-fold lower concentrations than VEGFR2, FGFR2, and JAK2, respectively.

Certain RET fusion proteins and activating point mutations can drive tumorigenic potential through hyperactivation of downstream signaling pathways leading to uncontrolled cell proliferation. Pralsetinib exhibited anti-tumor activity in cultured cells and animal tumor implantation models harboring oncogenic RET fusions or mutations including KIF5B-RET, CCDC6-RET, RET M918T, RET C634W, RET V804E, RET V804L and RET V804M. In addition, pralsetinib prolonged survival in mice implanted intracranially with tumor models expressing KIF5B-RET or CCDC6- RET.

**The products protected by patents in this product catalog are used for laboratory analysis, research and development, and cannot be sold to any country or region with patent protection and for commercial purpose. If the resulting patent infringement risks and responsibilities will be borne by the buyer.
Active Ingredient Dosage Form; Route Strength Proprietary Name Applicant
Patent Data
Patent No. Patent Expiration Drug Substance Claim Drug Product Claim Patent Use Code
Exclusive Data
Exclusivity Code Exclusivity Expiration
NCE 09/04/2025