MGCD0103

• CAT Number: I004705
• CAS Number: 726169-73-9
• Molecular Formula: C₂₃H₂₀N₆O
• Molecular Weight: 396.44
• Purity: ≥95%
• Target: HDAC inhibitor
• Solubility: Soluble in DMSO, not in water
• Storage: -20°C
• IC50: 0.15 μM(HDAC 1); 0.29 μM(HDAC 2); 1.66 μM(HDAC 3)
• 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

MGCD0103 (CAT: 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.

Overview of Clinical Research

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

Reference

1. Curr Opin Investig Drugs. 2007 Jun;8(6):485-92.

Drug evaluation: MGCD-0103, a histone deacetylase inhibitor for the treatment of
cancer.

Kell J(1).

Author information:
(1)Address University Hospital of Wales, Heath Park, Cardiff CF14 4XN, UK.


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.