ECF506-d5

ECF506-d5 (NXP900-d5) is deuterated labeled eCF506. eCF506 is a highly potent and orally active YES1/SRC kinase inhibitor with an IC50 of 0.47 nM. eCF506 locks its target into its native “closed” conformation, thereby inhibiting both kinase activity and complex formation with protein partners. eCF506 can be used for the study of esophageal squamous cancer and breast cancer[1][2][3].

Product Specifications

Product Name Alternative

NXP900-d5

UNSPSC

12352005

Target

Isotope-Labeled Compounds; Src

Type

Isotope-Labeled Compounds

Related Pathways

Others; Protein Tyrosine Kinase/RTK

Applications

Cancer-Kinase/protease

Field of Research

Cancer

Solubility

10 mM in DMSO

Smiles

[2H]C1(CN(CC([2H])(C1(N(C)C)[2H])[2H])CCN2N=C(C(C2=NC=N3)=C3N)C4=CC=C(C(OC)=C4)NC(OC(C)(C)C)=O)[2H]

Molecular Formula

C26H33D5N8O3

Molecular Weight

515.66

References & Citations

[1]Fraser C, et al. Rapid Discovery and Structure-Activity Relationships of Pyrazolopyrimidines That Potently Suppress Breast Cancer Cell Growth via SRC Kinase Inhibition with Exceptional Selectivity over ABL Kinase. J Med Chem. 2016 May 26;59 (10) :4697-710.|[2]Russak EM, et al. Impact of Deuterium Substitution on the Pharmacokinetics of Pharmaceuticals. Ann Pharmacother. 2019 Feb;53 (2) :211-216.|[3]Authors: Sweta Dash, et al. Preclinical efficacy of NXP900, a YES1/SRC kinase inhibitor in esophageal squamous cancer models. Journal of Clinical Oncology. Volume 41, Number 16_suppl.