2216753-97-6
Chemical Structure
Zeteletinib
Synonym(s): BOS-172738; DS-5010
- CAS No.: 2216753-97-6
- Formula:C25H23F3N4O4
- Molecular Weight:500.47
IUPAC Name: 2-(6-(6,7-dimethoxyquinolin-3-yl)pyridin-3-yl)-N-(3-(1,1,1-trifluoro-2-methylpropan-2-yl)isoxazol-5-yl)acetamide
InChIKey: KOLQINCWMXQEOF-UHFFFAOYSA-N
SMILES: O=C(CC1=CC=C(C2=CN=C3C=C(C(OC)=CC3=C2)OC)N=C1)NC4=CC(C(C)(C(F)(F)F)C)=NO4
Biological Activity: 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].
| Cat. No. | Product Name | Purity | Description | Pricing | |||||||||||||||||||
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Zeteletinib | 98.31% | 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. | ||||||||||||||||||||
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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. [Content Brief]
