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LAQ824 (NVP-LAQ824,Dacinostat)

Catalog No.
A4103
HDAC抑制剂
组合的产品项目
规格价格库存 数量
10mM (in 1mL DMSO)
¥ 1,980.00
现货
10mg
¥ 1,800.00
现货
50mg
¥ 4,700.00
现货
200mg
¥ 11,800.00
现货

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Background

LAQ824 (also known as NVP-LAQ824 or Dacinostat), a derivative of 4-aminomethylcinnamic hydroxamic acid, is a novel and potent inhibitor of histone deacetylase (HDAC) that inhibits the activity of HDAC with 50% inhibition concentration IC50 value of 0.03 μM. LAQ824 has been found to inhibit the growth of a variety of cancer cell lines, including colon cancer H1299 and HCT116 cells, breast cancer MDA435 cells, prostate cancer DU145 and PC3 cells and non-small cell lung cancer A549 cells, with IC50 value < 1 μM and induce apoptosis in human breast cancer SKBR-3, BT-474 and MB-468 cells. LAQ824 also dose- and time-dependently inhibits the growth of multiple myeloma cells.

Reference

Catley L, Weisberg E, Tai YT, Atadja P, Remiszewski S, Hideshima T, Mitsiades N, Shringarpure R, LeBlanc R, Chauhan D, Munshi NC, Schlossman R, Richardson P, Griffin J, Anderson KC. NVP-LAQ824 is a potent novel histone deacetylase inhibitor with significant activity against multiple myeloma. Blood. 2003 Oct 1;102(7):2615-22. Epub 2003 Jun 19.

文献引用

Chemical Properties

Physical AppearanceA solid
StorageStore at -20°C
M.Wt379.46
Cas No.404951-53-7
FormulaC22H25N3O3
SynonymsLAQ-824, NVP-LAQ 824
Solubility≥17.45 mg/mL in DMSO,insoluble in EtOH,insoluble in H2O
Chemical Name(E)-N-hydroxy-3-[4-[[2-hydroxyethyl-[2-(1H-indol-3-yl)ethyl]amino]methyl]phenyl]prop-2-enamide
SDFDownload SDF
Canonical SMILESC1=CC=C2C(=C1)C(=CN2)CCN(CCO)CC3=CC=C(C=C3)C=CC(=O)NO
运输条件试用装:蓝冰运输。 其他可选规格:常温运输或根据您的要求用蓝冰运输。
一般建议为了使其更好的溶解,请用37℃加热试管并在超声波水浴中震动片刻。不同厂家不同批次产品溶解度各有差异,仅做参考。若实验所需浓度过大至产品溶解极限,请添加助溶剂助溶或自行调整浓度。

试验操作

细胞实验[1]:

细胞系

Dexamethasone敏感的人多发性骨髓瘤(Dex-sensitive MM.1S)细胞

溶解方法

在DMSO中的溶解度>10 mM。为了获得更高的浓度,可以将离心管在37℃加热10分钟和/或在超声波浴中震荡一段时间。原液可以在-20℃以下储存几个月。

反应条件

20 nM;24、48或72 h

应用

作为HDAC的抑制剂,在常规疗法耐受的多发性骨髓瘤细胞系中,LAQ824诱导细胞凋亡。在该实验中,Dex(地塞米松)或LAQ824单独使用仅诱导15%和7%的生长抑制,而联合使用时,诱导51%的生长抑制。

动物实验[2]:

动物模型

经尾静脉注射植入32D.p210白血病细胞的雌性BALB/c小鼠

剂量

在植入白血病细胞后的3天,小鼠通过腹腔注射的方式每天给予25mg / kg的LAQ824或D5W对照。

应用

与对照相比,LAQ824治疗小鼠延迟了白血病和致死症状的发作。在LAQ824治疗小鼠和对照小鼠中,平均存活时间分别是20天和15.5天。

注意事项

请测试所有化合物在室内的溶解度,实际溶解度和理论值可能略有不同。这是由实验系统的误差引起的,属于正常现象。

References:

[1] Catley L, Weisberg E, Tai Y T, et al. NVP-LAQ824 is a potent novel histone deacetylase inhibitor with significant activity against multiple myeloma. Blood, 2003, 102(7): 2615-2622.

[2] Weisberg E, Catley L, Kujawa J, et al. Histone deacetylase inhibitor NVP-LAQ824 has significant activity against myeloid leukemia cells in vitro and in vivo. Leukemia, 2004, 18(12): 1951-1963.

生物活性

描述 LAQ824是一种新型的HDAC抑制剂,IC50值为32 nM。
靶点 HDAC          
IC50 32 nM          

质量控制

化学结构

LAQ824 (NVP-LAQ824,Dacinostat)

相关生物数据

LAQ824 (NVP-LAQ824,Dacinostat)