Dacinostat|404951-53-7|(达诺司他; NVP-LAQ824; LAQ824)-陌孚医药/Medlife

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Dacinostat (Synonyms: 达诺司他; NVP-LAQ824; LAQ824)

目录号: PL03545 纯度: ≥98%

CAS No. :404951-53-7

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中文名称	Dacinostat
中文别名	LAQ824 (Dacinostat) 抑制剂;LAQ-824 达诺斯他;达诺司他;达西司特;达诺斯他
英文名称	Dacinostat
英文别名	2-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;(E)-N-Hydroxy-3-[4-[[2-hydroxyethyl-[2-(1H-indol-3-yl)ethyl]amino]meth yl]phenyl]prop-2-enamide;(2E)-N-hydroxy-3-(4-{[(2-hydroxyethyl)[2-(1H-indol-3-yl)ethyl]amino]
Cas No.	404951-53-7
分子式	C₂₂H₂₅N₃O₃
分子量	379.45
包装储存	Powder -20°C 3 years；4°C 2 years

产品详情	Dacinostat 是一种有效的 HDAC 抑制剂，IC₅₀ 值为 32 nM；Dacinostat 同时可抑制 HDAC1 的活性，IC₅₀ 值为 9 nM，主要用于癌症研究。
生物活性	Dacinostat is a potent HDAC inhibitor, with an IC 50 of 32 nM; Dacinostat also inhibits HDAC1 with an IC 50 of 9 nM, and used in cancer research.
性状	Solid
IC50 & Target[1][2]	HDAC1 9 nM (IC50) HDAC 32 nM (IC50
体外研究(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. Dacinostat inhibits HDAC1 with an IC50 of 9 nM. Dacinostat (10 and 20 nM) suppresses prolifera
体内研究(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. has not independently confirmed the accuracy of these methods. They are for reference only.
运输条件	Room temperature in continental US; may vary elsewhere.
储存方式	Powder -20°C 3 years；4°C 2 years
参考文献	[1]. Atadja P, et al. Selective growth inhibition of tumor cells by a novel histone deacetylase inhibitor, NVP-LAQ824. Cancer Res. 2004 Jan 15;64(2):689-95. [2]. Cho YS, et al. Conformational refinement of hydroxamate-based histone deacetylase inhibitors and exploration of 3-piperidin-3-ylindole analogues of dacinostat (LAQ824). J Med Chem. 2010 Apr 8;53(7):2952-63.

溶解度数据	In Vitro: DMSO : ≥ 43 mg/mL (113.32 mM)配制储备液

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