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Dacinostat (NVP-LAQ824, LAQ824) — Datasheet

CAT. NO. DC7182

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ParameterValue
Chemical NameDacinostat free base
CAS No.404951-53-7
Synonyms2-Propenamide,N-hydroxy-3-[4-[[(2-hydroxyethyl)[2-(1H-indol-3-yl)ethyl]amino]methyl]phenyl]-,(2E)-;(E)-N-hydroxy-3-[4-[[2-hydroxyethyl-[2-(1H-indol-3-yl)ethyl]amino]methyl]phenyl]prop-2-enamide;2-Propenamide,N-hydroxy-3-[4-[[(2-hydroxyethyl)[2-(1H-indol-3-yl)ethyl]amino]methyl]phenyl]-,(...;Dacinostat;LAQ824;LAQ824 (Dacinostat);LAQ824 (NVP-LAQ824);LAQ824 (NVP-LAQ824, Dacinostat);LAQ-824;NVP-LAQ824;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)-;V10P524501;(2E)-N-hydroxy-3-(4-{[(2-hydroxyethyl)[2-(1H-indol-3-yl)ethyl]amino]methyl}phenyl)prop-2-enamide;Dacinostat [INN];(E)-N-Hydroxy-3-[4-[[2-hydroxyethyl-[2-(1H-indol-3
FormulaC22H25N3O3
M.Wt379.45
SMILESO([H])C([H])([H])C([H])([H])N(C([H])([H])C1C([H])=C([H])C(/C(/[H])=C(\[H])/C(N([H])O[H])=O)=C([H])C=1[H])C([H])([H])C([H])([H])C1=C([H])N([H])C2=C([H])C([H])=C([H])C([H])=C12
Purity>98%
Storage2 years -20°C Powder, 2 weeks 4°C in DMSO, 6 months -80°C in DMSO

Biological Activity

Dacinostat is a potent HDAC inhibitor, with an IC50 of 32 nM; Dacinostat also inhibits HDAC1 with an IC50 of 9 nM, and used in cancer research.

In Vitro

Dacinostat (NVP-LAQ824) activates p21 promoter, with AC50 of 0.30 μM. NVP-LAQ824 inhibits tumor cell (H1299, HCT116) growth, with IC50s of 150 and 10 nM, respectively. NVP-LAQ824 also shows inhibitory activities against two prostate cancer cell lines (DU145 and PC3) and a breast cancer line (MDA435), with IC50s of 18, 23, 39 nM, respectively. Continuous exposure of NVP-LAQ824 for 72 h produces LD90s of 0.09 M in HCT116 cells and 0.47 M in A549 cells. NVP-LAQ824 treatment of NDHF cells causes the expected G1-S growth arrest in addition to a significant reduction of cells in S-phase and accumulation of cells at the G2-M checkpoint. NVP-LAQ824 induces apoptotic death in human tumor cells. NPV-LAQ824 increases acetylation of histones H3 and H4[1]. Dacinostat inhibits HDAC1 with an IC50 of 9 nM[2]. Dacinostat (10 and 20 nM) suppresses proliferation of AML fusion protein-expressing 32D cells. Dacinostat impairs short-term engraftment potential of leukemic stem cells. Dacinostat exhausts in vitro self-renewal potential of murine AML1/ETO- and PLZF/RARα-positive HSC[3].

In Vivo

NVP-LAQ824 produces a dose-dependent inhibition of tumor growth, and at 100 mg/kg, its antitumor effect is similar to that of 5-Fluorouracil[1].

References & source

DC Chemicals original product information

Published experimental findings depend on the model and assay conditions. They do not guarantee equivalent performance in every application. For laboratory research use only.

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