Mocetinostat (MGCD0103) is a potent and isotype-selective inhibitor of histone deacetylases (HDACs). In cell-free assays, Mocetinostat (MGCD0103) exhibited most potent inhibition against human HDAC1 (IC50 = 0.15 ?M) and also has inhibitory activity against HDAC2, HDAC3, and HDAC11, with IC50 values ranged 0.3 to 1.7 ?M. No activity was showed on HDACs 4-8. [1] Mocetinostat (MGCD0103) exhibited potent inhibition activity in proliferation of human cancer cell lines, both in cell-based assay and in human tumor xenografts in nude mice. [1]
Mocetinostat (MGCD0103) has been evaluated in Phase II clinical trials in patients with metastatic leiomyosarcoma [2] and Hodgkin??s lymphoma [3]."
Technical information:
| Chemical Formula: | C23H20N6O | |
| CAS #: | 726169-73-9 | |
| Molecular Weight: | 396.44 | |
| Purity: | > 98% | |
| Appearance: | Off-white | |
| Chemical Name: | N-(2-aminophenyl)-4-((4-(pyridin-3-yl)pyrimidin-2-ylamino)methyl)benzamide | |
| Solubility: | Up to 10 mM in DMSO | |
| Synonyms: | Mocetinostat, MGCD0103, MG0103 |
Shipping Condition: The product is shipped in a glass vial at ambient temperature.
Storage condition: For longer shelf life, store solid powder or DMSO solution at -20oC desiccated.
Reference:
| 1. | Fournel M, 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):759-68 Pubmed ID: 18413790 |
| 2. | SARC018: A Study of Mocetinostat and Gemcitabine in Patients With Metastatic Leiomyosarcoma. clinicaltrials.gov/NCT02303262 |
| 3. | Mocetinostat (MGCD0103) Plus Brentuximab Vedotin (SGN-35) in Patients With Relapsed or Refractory Hodgkin Lymphoma. clinicaltrials.gov/NCT02429375 |
Other Information:
Product Specification (pdf)
MSDS (pdf)
Certificate of Analysis is available upon request.