2. Protein Tyrosine Kinase/RTK
  3. RET PDGFR
  4. Zeteletinib hemiadipate

Zeteletinib hemiadipate  (Synonyms: BOS-172738 hemiadipate; DS-5010 hemiadipate)

Cat. No.: HY-139590A
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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.

For research use only. We do not sell to patients.

Zeteletinib hemiadipate Chemical Structure

Zeteletinib hemiadipate Chemical Structure

CAS No. : 2375837-06-0

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Zeteletinib hemiadipate Related Antibodies

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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].

IC50 & Target[1]

PDGFR2

 

In Vitro

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 IC50 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].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Zeteletinib hemiadipate Related Antibodies
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 IC50 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].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Clinical Trial
Molecular Weight

573.55

Formula

C25H23F3N4O4.1/2C6H10O4
CAS No.
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]
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Room temperature in continental US; may vary elsewhere.
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Please store the product under the recommended conditions in the Certificate of Analysis.
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Zeteletinib hemiadipate Related Classifications

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  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

Zeteletinib hemiadipate2375837-06-0BOS-172738 hemiadipateDS-5010 hemiadipateRETPDGFRPlatelet-derived growth factor receptororallyRETV804M/LM918TInhibitorinhibitorinhibit

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