Powder: -20°C for 3 years | In solvent: -80°C for 1 year
Zeteletinib hemiadipate (BOS-172738; DS-5010) is an orally active compound that functions as a selective inhibitor of RET kinase. It exhibits nanomolar potency against RET and a 300-fold selectivity towards VEGFR2. Notably, Zeteletinib hemiadipate demonstrates exceptional effectiveness against various forms of RET, including the wild type, RET V804M/L gatekeeper mutants, and the oncogenic RET mutation M918T. Additionally, Zeteletinib hemiadipate exerts potent antitumor effects.
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5 mg | Inquiry | $ 970.00 |
Description | Zeteletinib hemiadipate (BOS-172738; DS-5010) is an orally active compound that functions as a selective inhibitor of RET kinase. It exhibits nanomolar potency against RET and a 300-fold selectivity towards VEGFR2. Notably, Zeteletinib hemiadipate demonstrates exceptional effectiveness against various forms of RET, including the wild type, RET V804M/L gatekeeper mutants, and the oncogenic RET mutation M918T. Additionally, Zeteletinib hemiadipate exerts potent antitumor effects. |
In vitro | In biochemical assays involving 106 kinases, Zeteletinib hemiadipate (BOS-172738; DS-5010) demonstrated significant inhibitory activity, surpassing 80% inhibition at 193 nM for both RET and platelet-derived growth factor receptor (PDGFR) alpha/beta. Furthermore, Zeteletinib displayed potent efficacy against RET and RET-GKm (V804L), with IC50 values in the single-digit nanomolar range, even in the presence of a high ATP concentration. Conversely, its inhibitory effect on KDR exceeded 1000 nM[1]. |
In vivo | 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 IC 50 values 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]. |
Synonyms | BOS-172738 hemiadipate, DS-5010hemiadipate, Zeteletinib hemiadipate |
Molecular Weight | 1147.098 |
Formula | C56H56F6N8O12 |
CAS No. | 2375837-06-0 |
Powder: -20°C for 3 years | In solvent: -80°C for 1 year
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