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Mocetinostat
- MGCD 0103 - MG 0103
- Soluble in 0.1N HCl(aq) and DMSO
- MF: C23H20N6O
- MW: 396.44
Description
Class I selective HDAC inhibitor (sub-micromolar IC50 values for HDAC1, HDAC2, and HDAC11, ca 2 μM for HDAC3, and >10 μM for HDAC4-8) with broad spectrum antitumor activity in vitro and in vivo. MGCD 0103 induced hyperacetylation of histones, selectively induced apoptosis, caused cell cycle blockade, and exhibited potent and selective antiproliferative activities against a broad spectrum of human cancer cell lines in vitro.
More Information
| Parent CAS No. | 726169-73-9 |
|---|---|
| Chemical Name | N-(2-aminophenyl)-4-((4-(pyridin-3-yl)pyrimidin-2-ylamino)methyl)benzamide |
| SMILES | C(NC1=CC=CC=C1N)(=O)C1=CC=C(CNC2=NC=CC(C3=CC=CN=C3)=N2)C=C1 |
| MFCD | N.A. |
| InChi | InChI=1S/C23H20N6O/c24-19-5-1-2-6-21(19)28-22(30)17-9-7-16(8-10-17)14-27-23-26-13-11-20(29-23)18-4-3-12-25-15-18/h1-13,15H,14,24H2,(H,28,30)(H,26,27,29) |
| InChiKey | HRNLUBSXIHFDHP-UHFFFAOYSA-N |
| CID | 9865515 |
| Short Description | HDAC inhibitor |
References
- T. Beckers et al. Distinct pharmacological properties of second generation HDAC inhibitors with the benzamide or hydroxamate head group. Int J Cancer. 2007 Sep 1;121(5):1138-48.
- M. Fournel et al. MGCD0103, a novel isotype-selective histone deacetylase inhibitor, has broad spectrum antitumor activity in vitro and in vivo. Mol Cancer Ther. 2008 Apr;7(4):759-68.
- N. Zhou et al. Discovery of N-(2-aminophenyl)-4-[(4-pyridin-3-ylpyrimidin-2-ylamino)methyl]benzamide (MGCD0103), an orally active histone deacetylase inhibitor. J Med Chem. 2008 Jul 24;51(14):4072-5.
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