HDAC Inhibitors

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MGCD0103

MGCD0103 (Mocetinostat) is an isotype-selective HDAC inhibitor, which primarily targets human HDAC1 and HDAC2 enzymes with weaker inhibition of HDAC3 and HDAC11 and does not inhibit HDAC4, HDAC5, HDAC6, HDAC7 or HDAC8.

MGCD0103

IUPAC Name: N-(2-aminophenyl)-4-[[(4-pyridin-3-ylpyrimidin-2-yl)amino]methyl]benzamide
Molecular Weight: 396,46 g/mol
Molecular Formula: C23H20N6O
SMILES: Nc1ccccc1NC(=O)c(cc4)ccc4CNc2nccc(n2)-c3cccnc3
Canonical SMILES: C1=CC=C(C(=C1)N)NC(=O)C2=CC=C(C=C2)CNC3=NC=CC(=N3)C4=CN=CC=C4
InChIKey Identifier: HRNLUBSXIHFDHP-UHFFFAOYSA-N
CAS Number: 726169-73-9
Melting point: n/a °C
Solubility: : soluble in DMSO
2D Molfile: Get the molfile
Synonyms: Mocetinostat; MGCD-0103

MGCD0103 has been evaluated in multiple Phase I and Phase II clinical trials in both solid tumor and hematological cancers and has demonstrated both single-agent and combination activity.

References:
1) Marielle Fournel, Claire Bonfils, Yu Hou, Pu Theresa Yan et al. MGCD0103, a novel isotype-selective histone deacetylase inhibitor, has broad spectrum antitumor activity in vitro and in vivo. Mol Cancer Ther 2008;7(4).
2) Daniel Riester, Christian Hildmann, Andreas Schwienhorst. Histone deacetylase inhibitors - turning epigenic mechanisms of gene regulation into tools of therapeutic intervention in malignant and other diseases. Appl Microbiol Biotechnol (2007) 75:499514
3) Tan J, Cang S, Ma Y, Petrillo RL, Liu D. Novel histone deacetylase inhibitors in clinical trials as anti-cancer agents. J Hematol Oncol. 2010 Feb 4;3(1):5.

HDACs


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