Entinostat-d₄  (Synonyms: MS-275-d₄; SNDX-275-d₄)

Entinostat-d₄ is the deuterium labeled Entinostat[1]. Entinostat is an oral and selective class I HDAC inhibitor, with IC50s of 243 nM, 453 nM, and 248 nM for HDAC1, HDAC2, and HDAC3, respectively[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].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

380.43

C₂₁H₁₆D₄N₄O₃

209783-80-2

Solid

O=C(NCC1=CC=C(C=C1)C(NC2=C([2H])C([2H])=C([2H])C([2H])=C2N)=O)OCC3=CC=CN=C3

Room temperature in continental US; may vary elsewhere.

• [1]. Russak EM, et al. Impact of Deuterium Substitution on the Pharmacokinetics of Pharmaceuticals. Ann Pharmacother. 2019 Feb;53(2):211-216.  [Content Brief]

  [2]. Lauffer BE, et al. Histone deacetylase (HDAC) inhibitor kinetic rate constants correlate with cellular histone acetylation but not transcription and cell viability. J Biol Chem. 2013 Sep 13;288(37):26926-43.  [Content Brief]