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Zeteletinib

Catalog No. T39688 CAS 2216753-97-6

Synonyms: BOS-172738, DS-5010, Zeteletinib

Zeteletinib (BOS-172738; DS-5010) is a highly potent and selective orally active inhibitor of the RET kinase. It demonstrates nanomolar potency against RET while exhibiting over 300-fold selectivity against VEGFR2. Zeteletinib exhibits remarkable efficacy against the wild-type RET, RET V804M/L gatekeeper mutants, as well as the frequently occurring oncogenic RET mutation M918T. Its antitumor activity is potent.

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Zeteletinib, CAS 2216753-97-6

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Description	Zeteletinib (BOS-172738; DS-5010) is a highly potent and selective orally active inhibitor of the RET kinase. It demonstrates nanomolar potency against RET while exhibiting over 300-fold selectivity against VEGFR2. Zeteletinib exhibits remarkable efficacy against the wild-type RET, RET V804M/L gatekeeper mutants, as well as the frequently occurring oncogenic RET mutation M918T. Its antitumor activity is potent.
In vitro	In biochemical assays involving 106 kinases, Zeteletinib (BOS-172738; DS-5010) achieved more than 80% inhibition of RET and platelet-derived growth factor receptor (PDGFR) alpha/beta at a concentration of 193 nM. Zeteletinib displayed potent activity against RET and RET-GKm (V804L) with IC50 values in the single-digit nanomolar range, even in the presence of high ATP concentrations. Conversely, its inhibitory effect on KDR exceeded 1000 nM[1].
In vivo	In a Ba/F3-RET subcutaneous tumor model, Zeteletinib (BOS-172738; DS-5010) administered at 10 mg/kg twice daily (bid) effectively induces tumor regression[1]. Similarly, in an LC2/ad NSCLC xenograft model harboring the RET-CCDC6 fusion gene, a dosage regimen of Zeteletinib at 1 mg/kg three times daily (tid) has been shown to induce tumor regression[1].

Synonyms	BOS-172738, DS-5010, Zeteletinib
Molecular Weight	500.478
Formula	C25H23F3N4O4
CAS No.	2216753-97-6

Storage

Powder: -20°C for 3 years | In solvent: -80°C for 1 year

References and Literature

1. Yasuyuki Kaneta, et al.Abstract B173: Preclinical characterization and antitumor efficacy of DS-5010, a highly potent and selective RET inhibitor. MOLECULAR CANCERTHERAPEUTICS. January 2018, Volume 17, Issue 1. 2. Patrick Schoffski, et al. BOS172738, a highly potent and selective RET inhibitor, for the treatment of RET-altered tumors including RET-fusion+ NSCLC and RET-mutant MTC: Phase 1 study results. Journal of Clinical Oncology 39, no. 15_suppl (May 20, 2021) 3008-3008. 3. Kyaw Z Thein, et al. Precision therapy for RET-altered cancers with RET inhibitors. Trends Cancer. 2021 Dec;7(12):1074-1088.

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Please see Inhibitor Handling Instructions for more frequently ask questions. Topics include: how to prepare stock solutions, how to store products, and cautions on cell-based assays & animal experiments, etc.

Keywords

Zeteletinib 2216753-97-6 BOS172738 DS5010 BOS-172738 DS 5010 DS-5010 BOS 172738 inhibitor inhibit

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