Prexasertib-d4
Prexasertib-d4 (LY2606368-d4) is the deuterium labeled Prexasertib (HY-18174). Prexasertib (LY2606368) is a selective, ATP-competitive second-generation checkpoint kinase 1 (CHK1) inhibitor with a Ki of 0.9 nM and an IC50 of <1 nM. Prexasertib inhibits CHK2 (IC50=8 nM) and RSK1 (IC50=9 nM). Prexasertib causes double-stranded DNA breakage and replication catastrophe resulting in apoptosis. Prexasertib shows potent anti-tumor activity.
For research use only. We do not sell to patients.
- Formula: C18H15D4N7O2
- Molecular Weight:369.41
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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.
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 1234015-52-1
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Molecular Weight 369.41
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Formula C18H15D4N7O2
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SMILES
NC([2H])([2H])CC([2H])([2H])OC(C=CC=C1OC)=C1C2=CC(NC3=NC=C(C#N)N=C3)=NN2
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Synonyms
LY2606368-d4
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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]. King C, et al. LY2606368 Causes Replication Catastrophe and Antitumor Effects through CHK1-Dependent Mechanisms. Mol Cancer Ther. 2015 Sep;14(9):2004-1 [Content Brief]
[2]. Yin Y, et al. Chk1 inhibition potentiates the therapeutic efficacy of PARP inhibitor BMN673 in gastric cancer. Am J Cancer Res. 2017 Mar 1;7(3):473-483. [Content Brief]
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)