MGCD0103

For research use only. Not for therapeutic Use.

  • CAT Number: I004705
  • CAS Number: 726169-73-9
  • Molecular Formula: C₂₃H₂₀N₆O
  • Molecular Weight: 396.44
  • Purity: ≥95%
Inquiry Now

MGCD0103 (Cat No.:I004705) is a small-molecule inhibitor that targets histone deacetylases (HDACs). HDACs are enzymes involved in the regulation of gene expression by removing acetyl groups from histone proteins, leading to chromatin compaction and gene silencing. MGCD0103 specifically inhibits HDAC1, HDAC2, and HDAC3 isoforms, resulting in the accumulation of acetyl groups on histones and the activation of gene transcription. This compound has shown potential as an anticancer agent, particularly in hematological malignancies and solid tumors. MGCD0103 is being investigated for its ability to induce cell cycle arrest, promote apoptosis, and inhibit tumor growth. It represents a promising therapeutic option in the field of epigenetic cancer therapy.


Catalog Number I004705
CAS Number 726169-73-9
Synonyms

Mocetinostat; MGCD-0103; N-(2-aminophenyl)-4-[[(4-pyridin-3-ylpyrimidin-2-yl)amino]methyl]benzamide

Molecular Formula C₂₃H₂₀N₆O
Purity ≥95%
Target Epigenetics
Solubility Soluble in DMSO, not in water
Storage -20°C
Overview of Clinical Research

Originator: MethylGene<br />
Developer: MedImmune; MethylGene; Mirati Therapeutics<br />
Class: Antineoplastics; Benzamides; Pyrimidines; Small molecules<br />
Mechanism of Action: Histone deacetylase inhibitors<br />
Orphan Drug Status Yes: – Acute myeloid leukaemia; Myelodysplastic syndromes; Hodgkin/’s disease; Diffuse large B cell lymphoma<br />
New Molecular Entity: Yes<br />

IC50 0.15 μM(HDAC 1); 0.29 μM(HDAC 2); 1.66 μM(HDAC 3)
IUPAC Name N-(2-aminophenyl)-4-[[(4-pyridin-3-ylpyrimidin-2-yl)amino]methyl]benzamide
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
SMILES C1=CC=C(C(=C1)N)NC(=O)C2=CC=C(C=C2)CNC3=NC=CC(=N3)C4=CN=CC=C4
Reference

1. Curr Opin Investig Drugs. 2007 Jun;8(6):485-92.
<br>
Drug evaluation: MGCD-0103, a histone deacetylase inhibitor for the treatment of
cancer.
<br>
Kell J(1).
<br>
Author information: <br>
(1)Address University Hospital of Wales, Heath Park, Cardiff CF14 4XN, UK.
[email protected]
<br>
MethylGene Inc, in collaboration with Pharmion Corp, is developing the
small-molecule, isoform-selective compound MGCD-0103 in North America for the
potential treatment of cancer. MGCD-0103 is currently undergoing phase II
clinical trials in patients with lymphoma, leukemia, myelodysplastic syndromes
and solid tumors, including pancreatic carcinoma. Taiho Pharmaceutical Co Ltd is
evaluating MGCD-0103 for oncological indications in South East Asia.

Request a Quote