Mocetinostat (MGCD0103, MG0103)
(Synonyms: N-(2-氨基苯基)-4-([[4-(吡啶-3-基)嘧啶-2-基]氨基]甲基)苯甲酰胺,MGCD-0103) 目录号 : GC13055
An orally available HDAC inhibitor
Cas No.:726169-73-9
Sample solution is provided at 25 µL, 10mM.
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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
[1].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
| Cell experiment: [1] | |
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Cell lines |
A549 cells |
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Preparation method |
The solubility of this compound in DMSO is >10 mM. General tips for obtaining a higher concentration: Please warm the tube at 37 °C for 10 minutes and/or shake it in the ultrasonic bath for a while.Stock solution can be stored below -20°C for several months. |
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Reaction Conditions |
50 μM, 16 hours |
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Applications |
MGCD0103 showed dose-dependent inhibition of HDAC activity in whole cells. At high concentrations in A549 cells, MGCD0103 inhibited a maximum of 80% of total activity. Cells were then subsequently washed with drug-free media. The inhibitory activity of MGCD0103 was sustained at least 48 hours after drug removal followed by a slow reversal. |
| Animal experiment: [1] | |
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Animal models |
Female CD-1 nude mice injected with A549 cells |
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Dosage form |
Oral administration, 120 mg/kg |
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Applications |
Administration of MGCD0103 (2HBr salt) significantly reduced growth of implanted advanced A549 tumors in nudemice in a dose-dependent manner after 13 days of daily administration. MGCD0103 (170 mg/kg for 2HBr salt, corresponding to 120 mg/kg of free base) significantly blocked growth of tumors compared with vehicle treatment alone with no change in body weight. In addition, MGCD0103 did not reduce WBC counts and was well tolerated. |
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Other notes |
Please test the solubility of all compounds indoor, and the actual solubility may slightly differ with the theoretical value. This is caused by an experimental system error and it is normal. |
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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. | |
| Cas No. | 726169-73-9 | SDF | |
| 别名 | N-(2-氨基苯基)-4-([[4-(吡啶-3-基)嘧啶-2-基]氨基]甲基)苯甲酰胺,MGCD-0103 | ||
| 化学名 | N-(2-aminophenyl)-4-[[(4-pyridin-3-ylpyrimidin-2-yl)amino]methyl]benzamide | ||
| Canonical SMILES | C1=CC=C(C(=C1)N)NC(=O)C2=CC=C(C=C2)CNC3=NC=CC(=N3)C4=CN=CC=C4 | ||
| 分子式 | C23H20N6O | 分子量 | 396.44 |
| 溶解度 | ≥ 19.8 mg/mL in DMSO | 储存条件 | Store at -20°C |
| General tips | 请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液；一旦配成溶液，请分装保存，避免反复冻融造成的产品失效。 储备液的保存方式和期限：-80°C 储存时，请在 6 个月内使用，-20°C 储存时，请在 1 个月内使用。 为了提高溶解度，请将管子加热至37℃，然后在超声波浴中震荡一段时间。 |
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| Shipping Condition | 评估样品解决方案：配备蓝冰进行发货。所有其他可用尺寸：配备RT，或根据请求配备蓝冰。 | ||
| 制备储备液 | |||
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1 mg | 5 mg | 10 mg |
| 1 mM | 2.5224 mL | 12.6122 mL | 25.2245 mL |
| 5 mM | 0.5045 mL | 2.5224 mL | 5.0449 mL |
| 10 mM | 0.2522 mL | 1.2612 mL | 2.5224 mL |
| 第一步：请输入基本实验信息（考虑到实验过程中的损耗，建议多配一只动物的药量） | ||||||||||
| 给药剂量 | mg/kg |  |
动物平均体重 | g | |
每只动物给药体积 | ul | |
动物数量 | 只 |
| 第二步：请输入动物体内配方组成（配方适用于不溶于水的药物；不同批次药物配方比例不同，请联系GLPBIO为您提供正确的澄清溶液配方） | ||||||||||
| % DMSO % % Tween 80 % saline | ||||||||||
| 计算重置 | ||||||||||
计算结果:
工作液浓度： mg/ml；
DMSO母液配制方法： mg 药物溶于 μL DMSO溶液（母液浓度 mg/mL，
体内配方配制方法：取 μL DMSO母液，加入 μL PEG300，混匀澄清后加入μL Tween 80，混匀澄清后加入 μL saline，混匀澄清。
1. 首先保证母液是澄清的；
2.
一定要按照顺序依次将溶剂加入，进行下一步操作之前必须保证上一步操作得到的是澄清的溶液，可采用涡旋、超声或水浴加热等物理方法助溶。
3. 以上所有助溶剂都可在 GlpBio 网站选购。
Quality Control & SDS
- View current batch:
- Purity: >99.00%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
- Datasheet