PLX-4720-d7
PLX-4720-d7 is the deuterium labeled PLX-4720. PLX-4720 is a potent and selective inhibitor of?B-RafV600E?with?an IC50?of 13 nM in a cell-free assay, equally potent to c-Raf-1 (Y340D and Y341D mutations), and 10-fold selectivity for B-RafV600E than wild-type B-Raf[1][2].
Product Specifications
CAS Number
1304096-50-1
UNSPSC
12352005
Target
Isotope-Labeled Compounds; Raf
Type
Isotope-Labeled Compounds
Related Pathways
MAPK/ERK Pathway; Others
Applications
Cancer-Kinase/protease
Field of Research
Cancer
Solubility
10 mM in DMSO
Smiles
O=C(C1=C(C(NS(C([2H])([2H])C([2H])([2H])C([2H])([2H])[2H])(=O)=O)=CC=C1F)F)C(C2=C3)=CNC2=NC=C3Cl
Molecular Formula
C17H7D7ClF2N3O3S
Molecular Weight
420.87
References & Citations
[1]Russak EM, et al. Impact of Deuterium Substitution on the Pharmacokinetics of Pharmaceuticals. Ann Pharmacother. 2019;53 (2) :211-216.|[2]Tsai J, et al. Discovery of a selective inhibitor of oncogenic B-Raf kinase with potent antimelanoma activity. Proc Natl Acad Sci U S A, 2008, 105 (8), 3041-3046.|[3]Paraiso KH, et al. PTEN loss confers BRAF inhibitor resistance to melanoma cells through the suppression of BIM expression. Cancer Res, 2011, 71 (7), 2750-2760.|[4]Nucera C, et al. B-Raf (V600E) and thrombospondin-1 promote thyroid cancer progression. Proc Natl Acad Sci U S A, 2010, 107 (23), 10649-10654.|[5]Rizzolio S, et al. Neuropilin-1 upregulation elicits adaptive resistance to oncogene-targeted therapies. J Clin Invest. 2018 Aug 31;128 (9) :3976-3990.
Shipping Conditions
Room temperature
Scientific Category
Isotope-Labeled Compounds
Clinical Information
No Development Reported
Frequently Asked Questions
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