Dabrafenib-d9
Based on 1 Customer Validation
Dabrafenib-d9 is the deuterium labeled Dabrafenib. Dabrafenib (GSK2118436A) is an ATP-competitive inhibitor of Raf with IC50s of 5 nM and 0.6 nM for C-Raf and B-RafV600E, respectively.
For research use only. We do not sell to patients.
- CAS No.: 1423119-98-5
- Formula: C23H11D9F3N5O2S2
- Molecular Weight:528.62
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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].
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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CAS No. 1423119-98-5
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Unlabeled Cas 1195765-45-7
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Molecular Weight 528.62
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Formula C23H11D9F3N5O2S2
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SMILES
O=S(C1=C(F)C=CC=C1F)(NC2=CC=CC(C3=C(C4=NC(N)=NC=C4)SC(C(C([2H])([2H])[2H])(C([2H])([2H])[2H])C([2H])([2H])[2H])=N3)=C2F)=O
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Synonyms
GSK2118436A-d9; GSK2118436-d9
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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;53(2):211-216. [Content Brief]
[2]. Greger JG, et al. Combinations of BRAF, MEK, and PI3K/mTOR inhibitors overcome acquired resistance to the BRAF inhibitor GSK2118436 dabrafenib, mediated by NRAS or MEK mutations. Mol Cancer Ther, 2012, 11(4), 909-920. [Content Brief]
[3]. Lee S, et al. Anti-inflammatory effects of dabrafenib on polyphosphate-mediated vascular disruption. Chem Biol Interact. 2016 Jul 22. [Content Brief]
[4]. Jung B, et al. Anti-septic effects of dabrafenib on HMGB1-mediated inflammatory responses. BMB Rep. 2016 Apr;49(4):214-9. [Content Brief]
[5]. Alexander M Menzies, et al. Dabrafenib and its potential for the treatment of metastatic melanoma. Drug Des Devel Ther. 2012; 6: 391–405. [Content Brief]
[6]. Posobiec LM, et al. Early Vaginal Opening in Juvenile Female Rats Given BRAF-Inhibitor Dabrafenib Is Not Associated with Early Physiologic Sexual Maturation. Birth Defects Res B Dev Reprod Toxicol. 2015 Dec;104(6):244-52. [Content Brief]
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)