Vemurafenib-d5

Vemurafenib-d5 is the 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[1][4]. Vemurafenib induces cell autophagy[5].

Product Specifications

CAS Number

[1365986-90-8]

UNSPSC

12352005

Target

Autophagy; Isotope-Labeled Compounds; Raf

Type

Isotope-Labeled Compounds

Related Pathways

Autophagy; MAPK/ERK Pathway; Others

Applications

Cancer-Kinase/protease

Field of Research

Cancer

Solubility

10 mM in DMSO

Smiles

C(=O)(C=1C=2C(NC1)=NC=C(C2)C3=CC=C(Cl)C=C3)C4=C(F)C(NS(CC(C([2H])([2H])[2H])([2H])[2H])(=O)=O)=CC=C4F

Molecular Formula

C23H13D5ClF2N3O3S

Molecular Weight

494.95

References & Citations

[1]Russak EM, et al. Impact of Deuterium Substitution on the Pharmacokinetics of Pharmaceuticals. Ann Pharmacother. 2019;53 (2) :211-216.|[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.|[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.|[4]Prahallad A, et al. Unresponsiveness of colon cancer to BRAF (V600E) inhibition through feedback activation of EGFR. Nature, 2012, 483 (7387), 100-103.|[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.|[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.