| Identification | Back Directory | [Name]
3-Pyridineacetamide, 6-(6,7-dimethoxy-3-quinolinyl)-N-[3-(2,2,2-trifluoro-1,1-dimethylethyl)-5-isoxazolyl]- | [CAS]
2216753-97-6 | [Synonyms]
DS-5010
BOS-172738
Zeteletinib
Zeteletinib( BOS-172738)
3-Pyridineacetamide, 6-(6,7-dimethoxy-3-quinolinyl)-N-[3-(2,2,2-trifluoro-1,1-dimethylethyl)-5-isoxazolyl]- | [Molecular Formula]
C25H23F3N4O4 | [MOL File]
2216753-97-6.mol | [Molecular Weight]
500.47 |
| Chemical Properties | Back Directory | [Boiling point ]
661.1±55.0 °C(Predicted) | [density ]
1.330±0.06 g/cm3(Predicted) | [storage temp. ]
Store at -20°C | [form ]
Solid | [pka]
12.23±0.70(Predicted) | [color ]
White to light yellow |
| Hazard Information | Back Directory | [Uses]
Zeteletinib (BOS-172738; DS-5010) is an orally active, selective RET kinase inhibitor with nanomolar potency against RET and >300-fold selectivity against VEGFR2. Zeteletinib shows exquisite potency for the wild type RET, RETV804M/L gatekeeper mutants, and the most common oncogenic RET mutation M918T. Zeteletinib has potent antitumor activity[1][2][3]. | [in vivo]
In a Ba/F3-RET subcutaneous tumor model, Zeteletinib (BOS-172738; DS-5010) dosing at 10 mg/kg twice daily (bid) induces tumor regression[1].
In an LC2/ad NSCLC xenograft model, which has the RET-CCDC6 fusion gene, Zeteletinib dosing at 1 mg/kg thrice daily (tid) induced tumor regression[1].
| [IC 50]
PDGFR2 | [References]
[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. DOI:10.1016/j.trecan.2021.07.003 |
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