PLX-4720-d7 |
| カタログ番号GC62206 |
PLX-4720-d7 は、PLX-4720 とラベル付けされた重水素です。 PLX-4720 は B-RafV600E の強力かつ選択的な阻害剤であり、無細胞アッセイで IC50 は 13 nM であり、c-Raf-1（Y340D および Y341D 変異）に対しても同等に強力で、B-RafV600E に対して 10 倍の選択性があります。野生型 B-Raf よりも。
Products are for research use only. Not for human use. We do not sell to patients.
Cas No.: 1304096-50-1
Sample solution is provided at 25 µL, 10mM.
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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].
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].
[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.
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