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Mocetinostat (MGCD0103, MG0103)

现货
Catalog No.
A4089
HDAC抑制剂
组合的产品项目
规格价格库存 数量
10mM (in 1mL DMSO)
¥ 880.00
现货
5mg
¥ 840.00
现货
10mg
¥ 1,160.00
现货
25mg
¥ 2,280.00
Ship with 10-15 days

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Background

Mocetinostat, also known as MGCD0103 or MG0103, is an isotype-selective inhibitor of human histone deacetylases (HDAC), a family of enzymes involved in epigenetic regulation of gene transcription as well as cell proliferation, death and motility. Mocetinostat potently inhibits HDAC class I (HDAC1, HDAC2, and HDAC3) and class IV (HDAC11), with values of inhibition constant IC50 of 0.15 μmol/L, 0.29 μmol/L, 1.66 μmol/L, and 0.59 μmol/L respectively, rather than HDAC class II. Mocetinostat exerts anti-tumor activity against a broad range of human cancer cells through HDAC inhibition, in which it induces histone hyperacetylation and apoptosis and causes cell cycle blockade in a dose-dependent manner.

Reference

Fournel M, Bonfils C, Hou Y, Yan PT, Trachy-Bourget MC, Kalita A, Liu J, Lu AH, Zhou NZ, Robert MF, Gillespie J, Wang JJ, Ste-Croix H, Rahil J, Lefebvre S, Moradei O, Delorme D, Macleod AR, Besterman JM, Li Z. MGCD0103, a novel isotype-selective histone deacetylase inhibitor, has broad spectrum antitumor activity in vitro and in vivo. Mol Cancer Ther. 2008; 7(4): 759-768

文献引用

1.Topper MJ, Vaz M, et al. "Epigenetic Therapy Ties MYC Depletion to Reversing Immune Evasion and Treating Lung Cancer." Cell. 2017 Nov 30;171(6):1284-1300.e21. PMID:29195073
2.Bagnall NH, Hines BM, et al. "Insecticidal activities of histone deacetylase inhibitors against a dipteran parasite of sheep, Lucilia cuprina." Int J Parasitol Drugs Drug Resist. 2017 Apr;7(1):51-60. PMID:28110187

Chemical Properties

Physical AppearanceA solid
StorageStore at -20°C
M.Wt396.44
Cas No.726169-73-9
FormulaC23H20N6O
SynonymsMGCD-0103
Solubility≥19.8 mg/mL in DMSO, <2.48 mg/mL in EtOH, <2.49 mg/mL in H2O
Chemical NameN-(2-aminophenyl)-4-[[(4-pyridin-3-ylpyrimidin-2-yl)amino]methyl]benzamide
SDFDownload SDF
Canonical SMILESC1=CC=C(C(=C1)N)NC(=O)C2=CC=C(C=C2)CNC3=NC=CC(=N3)C4=CN=CC=C4
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

A549细胞

溶解方法

该化合物在DMSO中的溶解度大于10 mM。若配制更高浓度的溶液,一般步骤如下:请将试管置于37℃加热10分钟和/或将其置于超声波浴中震荡一段时间。原液于-20℃可放置数月

反应条件

50 μM,16 hours

实验结果

MGCD0103以剂量依赖性方式抑制全细胞中HDAC的活性。在A549细胞中,MGCD0103在高浓度时最大抑制总活性的80%。随后用无药物培养基洗涤细胞。去除药物后MGCD0103抑制活性至少维持48小时,然后缓慢逆转。

动物实验[1]:

动物模型

注射A549细胞的雌性CD-1裸鼠

剂量

口服,120 mg/kg

实验结果

在植入晚期A549肿瘤的裸鼠中,每日给药MGCD0103(2HBr盐)13天后, MGCD0103以剂量依赖性方式显著降低肿瘤生长。与对照组相比,MGCD0103(2HBr salt,170mg/kg;对应于游离碱,120 mg/kg)显著阻断肿瘤生长,不影响体重变化。此外,MGCD0103不影响WBC计数并且耐受性良好。

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] Fournel M, Bonfils C, Hou Y, et al. MGCD0103, a novel isotype-selective histone deacetylase inhibitor, has broad spectrum antitumor activity in vitro and in vivo. Molecular Cancer Therapeutics, 2008, 7(4): 759-768.

生物活性

描述 Mocetinostat (MGCD0103)是一种有效的HDAC抑制剂,对HDAC1的作用最强,IC50值为0.15 μM,比对HDAC2、3和11的选择性高2-10倍,对HDAC4、 5、6、7和8没有作用。
靶点 HDAC1 HDAC2 HDAC3      
IC50 0.15 μM 0.29 μM 1.66 μM      

质量控制

化学结构

Mocetinostat (MGCD0103, MG0103)

相关生物数据

Mocetinostat (MGCD0103, MG0103)

相关生物数据

Mocetinostat (MGCD0103, MG0103)

相关生物数据

Mocetinostat (MGCD0103, MG0103)

相关生物数据

Mocetinostat (MGCD0103, MG0103)