Pelitinib-d6

Pelitinib-d6 (EKB-569-d6) is the deuterium labeled Pelitinib. Pelitinib (EKB-569) is an irreversible inhibitor of EGFR with an IC50 of 38.5 nM; also slightly inhibits Src, MEK/ERK and ErbB2 with IC50s of 282, 800, and 1255 nM, respectively[1][2].

Product Specifications

CAS Number

[1325223-34-4]

UNSPSC

12352005

Target

EGFR; Isotope-Labeled Compounds; Src

Related Pathways

JAK/STAT Signaling; Others; 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(F)C=C3

Molecular Formula

C24H17D6ClFN5O2

Molecular Weight

473.96

References & Citations

[1]Russak EM, et al. Impact of Deuterium Substitution on the Pharmacokinetics of Pharmaceuticals. Ann Pharmacother. 2019;53 (2) :211-216.|[2]Torrance CJ, et al. Combinatorial chemoprevention of intestinal neoplasia. Nat Med. 2000 Sep;6 (9) :1024-8.|[3]Nunes M, et al. Phosphorylation of extracellular signal-regulated kinase 1 and 2, protein kinase B, and signal transducer and activator of transcription 3 are differently inhibited by an epidermal growth factor receptor inhibitor, EKB-569, in tumor cells and normal human keratinocytes. Mol Cancer Ther. 2004 Jan;3 (1) :21-7.