Vemurafenib-d7
Vemurafenib-d7 is deuterium labeled Vemurafenib. Vemurafenib (PLX4032) is a first-in-class, selective, potent inhibitor of B-RAF kinase, with IC50s of 31 and 48 nM for RAFV600E and c-RAF-1, respectively. Vemurafenib induces cell autophagy.
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- No. CAS: 1365986-73-7
- Fòrmula: C23H11D7ClF2N3O3S
- Peso molecular:496.97
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Almacenamiento:
Please store the product under the recommended conditions in the Certificate of Analysis.
Actividad biológica
Descripciòn
In Vitro
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.
Aplicación
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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No. CAS 1365986-73-7
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Unlabeled CAS 918504-65-1
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Peso molecular 496.97
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Fòrmula C23H11D7ClF2N3O3S
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SMILES
O=C(C1=C(C(NS(C([2H])([2H])C([2H])([2H])C([2H])([2H])[2H])(=O)=O)=CC=C1F)F)C2=CNC3=NC=C(C4=CC=C(C=C4)Cl)C=C23
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Synonyms
PLX4032-d7; RG7204-d7; RO5185426-d7
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Envío
Room temperature in continental US; may vary elsewhere.
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Almacenamiento
Please store the product under the recommended conditions in the Certificate of Analysis.
Pureza y Documentación
Referencias
[1]. Russak EM, et al. Impact of Deuterium Substitution on the Pharmacokinetics of Pharmaceuticals. Ann Pharmacother. 2019;53(2):211-216. [Content Brief]
[2]. Bollag G, et al. Clinical efficacy of a RAF inhibitor needs broad target blockade in BRAF-mutant melanoma. Nature, 2010, 467(7315), 596-599. [Content Brief]
[3]. Yang H, et al. RG7204 (PLX4032), a selective BRAFV600E inhibitor, displays potent antitumor activity in preclinical melanoma models. Cancer Res, 2010, 70(13), 5518-5527. [Content Brief]
[4]. Prahallad A, et al. Unresponsiveness of colon cancer to BRAF(V600E) inhibition through feedback activation of EGFR. Nature, 2012, 483(7387), 100-103. [Content Brief]
[5]. Shelledy L, et al. Vemurafenib: First-in-Class BRAF-Mutated Inhibitor for the Treatment of Unresectable or MetastaticMelanoma. J Adv Pract Oncol. 2015 Jul-Aug;6(4):361-5. [Content Brief]
[6]. Wang W, et al. Targeting Autophagy Sensitizes BRAF-Mutant Thyroid Cancer to Vemurafenib.J Clin Endocrinol Metab. 2017 Feb 1;102(2):634-643. [Content Brief]
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)