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Product Description
– Zeteletinib (BOS-172738; DS-5010) hemiadipate is an orally active, selective RET kinase inhibitor with nanomolar potency against RET and >300-fold selectivity against VEGFR2. Zeteletinib hemiadipate shows exquisite potency for the wild type RET, RETV804M/L gatekeeper mutants, and the most common oncogenic RET mutation M918T. Zeteletinib hemiadipate has potent antitumor activity[1][2][3].
Web ID
– HY-139590A
Shipping
– Room temperature
Applications
– Cancer-Kinase/protease
Molecular Formula
– C25H23F3N4O4.1/2C6H10O4
References
– [1]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.|[2]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. |[3]Kyaw Z Thein, et al. Precision therapy for RET-altered cancers with RET inhibitors. Trends Cancer. 2021 Dec;7(12):1074-1088.
CAS Number
– 2375837-06-0
Molecular Weight
– 573.55
SMILES
– O=C(O)CCCCC(O)=O.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.[1/2]
Clinical Information
– Phase 1
Research Area
– Cancer
Solubility
– 10 mM in DMSO
Target
– PDGFR;RET
Isoform
– PDGFR
Pathway
– Protein Tyrosine Kinase/RTK
Product type
– Reference compound
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