Neratinib-d6

Neratinib-d6 (HKI-272-d6) is the deuterium labeled Neratinib. Neratinib (HKI-272) is an orally available, irreversible tyrosine kinase inhibitor with IC50s of 59 nM and 92 nM for HER2 and EGFR, respectively.

Product Specifications

CAS Number

[1259519-18-0]

UNSPSC

12352005

Target

EGFR

Type

Isotope-Labeled Compounds

Related Pathways

JAK/STAT Signaling; Protein Tyrosine Kinase/RTK

Applications

Cancer-Kinase/protease

Field of Research

Cancer

Solubility

10 mM in DMSO

Smiles

N(C=1C2=C(C=C(OCC)C(NC(/C=C/CN(C([2H])([2H])[2H])C([2H])([2H])[2H])=O)=C2)N=CC1C#N)C3=CC(Cl)=C(OCC4=CC=CC=N4)C=C3

Molecular Formula

C30H23D6ClN6O3

Molecular Weight

563.08

References & Citations

[1]Russak EM, et al. Impact of Deuterium Substitution on the Pharmacokinetics of Pharmaceuticals. Ann Pharmacother. 2019;53 (2) :211-216.|[2]Rabindran SK, et al. Antitumor activity of HKI-272, an orally active, irreversible inhibitor of the HER-2 tyrosine kinase. Cancer Res, 2004, 64 (11), 3958-3965.|[3]Yoshioka T, et al. Antitumor activity of pan-HER inhibitors in HER2-positive gastric cancer. Cancer Sci. 2018 Apr;109 (4) :1166-1176.