eCF506-d5
eCF506-d5 (NXP900-d5) is deuterated labeled eCF506 (HY-112096). 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.
For research use only. We do not sell to patients.
- Formula: C26H33D5N8O3
- Molecular Weight:515.66
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Storage:
Please store the product under the recommended conditions in the Certificate of Analysis.
Biological Activity
Stable heavy isotopes of hydrogen, carbon, and other elements have been incorporated into drug molecules, largely as tracers for quantitation during the drug development process. Deuteration has gained attention because of its potential to affect the pharmacokinetic and metabolic profiles of drugs[1].
eCF506 induces a very potent antiproliferative effect in both MCF7 and MDA-MB-231 cells. eCF506 inhibits phosphorylation of SRC and FAK at low nanomolar levels, with complete inhibition observed at 100 nM. eCF506 significantly reduces cell motility at 10 nM as early as 6 h into the study, with equivalent efficacy to dasatinib. eCF506 exclusively inhibits SFK, with subnanomolar IC50 values against SRC and YES (IC50=0.5, 2.1 nM). It is important to highlight that eCF506 displays a vast difference in activity (>950-fold difference) between ABL and its primary target SRC[2].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
1. This compound can be used as a tracer
2. This compound can be used as an internal standard for quantitative analysis by NMR, GC-MS, or LC-MS.
Chemical Information
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Unlabeled Cas 1914078-41-3
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Molecular Weight 515.66
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Formula C26H33D5N8O3
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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]
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Synonyms
NXP900-d5
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Shipping
Room temperature in continental US; may vary elsewhere.
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Storage
Please store the product under the recommended conditions in the Certificate of Analysis.
Purity & Documentation
References
[1]. Russak EM, et al. Impact of Deuterium Substitution on the Pharmacokinetics of Pharmaceuticals. Ann Pharmacother. 2019 Feb;53(2):211-216. [Content Brief]
[2]. 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. [Content Brief]
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)