Mocetinostat (MGCD0103)
Mocetinostat (MGCD0103)
CAS: 726169-73-9
Molecular Formula: C23H20N6O
Mocetinostat (MGCD0103) - Names and Identifiers
Mocetinostat (MGCD0103) - Physico-chemical Properties
| Molecular Formula | C23H20N6O |
| Molar Mass | 396.44 |
| Density | 1.340±0.06 g/cm3(Predicted) |
| Melting Point | >170oC (dec.) |
| Solubility | DMSO 13 mg/mL (32.79 mM); Water <1 mg/mL (<1 mM); Ethanol <1 mg/mL (<1 mM) |
| Appearance | solid |
| Color | Off-white |
| pKa | 13.13±0.70(Predicted) |
| Storage Condition | RT |
| Stability | Stable for 1 year from date of purchase as supplied. Solutions in DMSO may be stored at -20°C for up to 2 months. |
| Use | A potent inhibitor of HDAC1, HDAC2, HDAC3, and HDAC11. |
| In vitro study | MGCD0103 inhibited only a portion of the nine human recombinant HDACs, including HDAC1, HDAC2, HDAC3, and HDAC11, in a dose-dependent manner at nanomolar or low micromolar concentrations. In vitro, MGCD0103 potently inhibits human HDAC1 and HDAC2 enzymes, but does not inhibit secondary HDACs. The exocyclic amino inhibitory enzyme of MGCD0103 is necessary because the HDAC inhibitory activity acting on HDAC1 and HDAC2 has been completely eliminated by desanino analogs. At 6 μm, the inhibitory activity of MGCD0103 reached the highest state. In HCT116 cells, MGCD0103 inhibited the total enzyme activity by 75%, while the inhibition by NVP-LAQ824 was almost 100%. MGCD0103 also showed dose-dependent inhibition of A549 cells. |
| In vivo study | In nude mice, MGCD0103 significantly inhibited the growth of human transplanted tumors and the related anticancer activity of histone acetylation induction in tumors. Oral daily treatment of MGCD0103 in nude mice carrying transplanted advanced A549 tumors significantly reduced growth after 13 days in a dose-dependent manner. MGCD0103 significantly blocked tumor growth and did not change body weight compared to the control group. In addition, MGCD0103 did not reduce WBC counts and was well tolerated. MGCD0103 is orally effective in a number of other human xenograft models, including NSCLC h1437. MGCD0103 was administered orally to H1437 tumor-bearing animals at a dose of 80 mg/kg daily. After 13 days, tumor growth was completely inhibited, and the animals did not lose weight. MGCD0103 is more effective in reducing pulmonary hypertension than tadalafil, a conventional treatment for pulmonary hypertension and a vasodilator. In addition, MGCD0103 increases the pulmonary artery acceleration time and reduces the contraction of the pulmonary artery, indicating that HDAC inhibitors have a good effect on pulmonary vessels. |
Mocetinostat (MGCD0103) - Introduction
Mocetinostat (MGCD0103) is a potent HDAC inhibitor with the strongest inhibitory effect on HDAC1, with an IC50 of 0.15 μM, which is 2 to 10 times more selective than HDAC2, 3, and 11, and has no inhibitory activity on HDAC4, 5, 6, 7, and 8. Phase 2.
Last Update：2022-10-16 17:41:48
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Product Name: Mocetinostat (MGCD0103) Visit Supplier Webpage Request for quotationCAS: 726169-73-9
Tel: 18301782025
Email: 3008007409@qq.com
Mobile: 18021002903
QQ: 3008007409
Wechat: 18301782025
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