Zeteletinib (BOS-172738; DS-5010) hemiadipate is an orally active, selectiveRETkinaseinhibitor with nanomolar potency againstRETand >300-fold selectivity against VEGFR2. Zeteletinib hemiadipate shows exquisite potency for the wild typeRET,RET^V804M/Lgatekeeper mutants, and the most common oncogenicRETmutationM918T. Zeteletinib hemiadipate has potent antitumor activity^[1][2][3].

In biochemical assays of 106 kinases, RET and platelet-derived growth factor receptor (PDGFR) alpha/beta were inhibited more than 80% by 193 nM Zeteletinib (BOS-172738; DS-5010) hemiadipate. The IC₅₀values of Zeteletinib hemiadipate against RET, RET-GKm (V804L) were single digit nano-molar even under a condition of high concentration of ATP; besides it against KDR was more than 1000 nM^[1].

In biochemical assays of 106 kinases, RET and platelet-derived growth factor receptor (PDGFR) alpha/beta were inhibited more than 80% by 193 nM Zeteletinib (BOS-172738; DS-5010) hemiadipate. The IC₅₀values of Zeteletinib hemiadipate against RET, RET-GKm (V804L) were single digit nano-molar even under a condition of high concentration of ATP; besides it against KDR was more than 1000 nM^[1].

573.55

C₂₅H₂₃F₃N₄O₄.1/2C₆H₁₀O₄

2375837-06-0

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