LAQ824 (Dacinostat)

Name	2-Propenamide, N-hydroxy-3-[4-[[(2-hydroxyethyl)[2-(1H-indol-3-yl)ethyl]amino]methyl]phenyl]-, (2E)-
Synonyms	LAQ-824 dacinostat Dacinostat LAQ824 (Dacinostat) Dacinostat(NVP-LAQ 824) (E)-3-(4-(((2-(1H-indol-3-yl)ethyl)(2-hydroxyethyl)amino)methyl)phenyl)-N-hydroxyacrylamide (E)-N-hydroxy-3-[4-[[2-hydroxyethyl-[2-(1H-indol-3-yl)ethyl]amino]meth yl]phenyl]prop-2-enamide 3-[4-[N-(2-Hydroxyethyl)-N-[2-(1H-indol-3-yl)ethyl]aminomethyl]phenyl]-2(E)-propenohydroxamic acid 2-Propenamide, N-hydroxy-3-[4-[[(2-hydroxyethyl)[2-(1H-indol-3-yl)ethyl]amino]methyl]phenyl]-, (2E)-
CAS	404951-53-7

Molecular Formula	C22H25N3O3
Molar Mass	379.45
Density	1.290±0.06 g/cm3(Predicted)
pKa	8.81±0.23(Predicted)
Storage Condition	2-8℃
In vitro study	In vitro, LAQ824 inhibited human HDAC activity in H1299 Cell Lysates with an IC50 of 32 nM. In addition, LAQ824 also activated the expression of a gene encoding a p21 cell cycle inhibitor by activating the p21 promoter at a concentration of 50% μm at a maximum promoter activity (AC50) of 0.30. After 72 hours of treatment, LAQ824 inhibited the growth of H1299 (a non-small cell lung cancer cell) and HCT116 (a colon cancer cell) cells with IC50 of 0.15 μM and 0.01 μm, respectively, the antiproliferative effect of LAQ824 selectively acts on tumor cell lines. Moreover, LAQ824 acts on A549 cells to promote the increase of p21 protein in a dose-dependent manner, and increases the hypophosphorylation state of Rb tumor suppressor gene. Recent studies have shown that LAQ824 induces chromosomal changes at the IL-10 gene promoter level, resulting in enhanced recruitment of transcription inhibitors HDAC11 and PU.1, and IL-10 inhibition of production in BALB/c macrophages.
In vivo study	LAQ824 inhibited tumor growth in nude mice bearing HCT116 and human colon cancer xenografts at a dose of 100 mg/kg without cytotoxicity in a dose-dependent manner.