864814-88-0
Resminostat
CAS: 864814-88-0
Molecular Formula: C16H19N3O4S
864814-88-0 - Names and Identifiers
864814-88-0 - Physico-chemical Properties
| Molecular Formula | C16H19N3O4S |
| Molar Mass | 349.4 |
| Density | 1.28±0.1 g/cm3(Predicted) |
| pKa | 8.68±0.23(Predicted) |
| Storage Condition | -20℃ |
| Use | Resminostat dose-dependent selective inhibition of HDAC1/3/6, IC50 is 42.5 nM/50.1 nM/71.8 nM, the effect on HDAC8 is weak, IC50 is 877 nM. |
| In vitro study | Resminostat[HCl], a potent inhibitor, is a recombinant of HDAC1,3 and 6 isozymes that competitively bind to the matrix. It acts on MM cells and can induce high acetylation of histone H4. Resminostat acts at low micromolar concentrations on MM cell lines (OPM-2,NCI-H929,U266) to prevent cell growth and strongly induce apoptosis, consistent with the effect on primary MM cells. At 1 μm, Resminostat acts on the MM cell line, inhibiting cell proliferation and inducing G0/G1 phase arrest of the cell cycle at OPM-2,NCI-H929, u266. The cell lines were accompanied by decreased levels of cyclin D1,CDC25A,CDK4 and Rb and up-regulation of the p21 gene. Resminostat directs interference with the Akt signaling pathway by reducing phosphorylation of 4E-BP1 and p70S6K. Treatment with Resminostat resulted in increased levels of Bim and Bax protein expression and a decrease of Bcl-xL levels. Resminostat activates Caspases 3, 8, and 9. In addition, Resminostat synergizes with Melphalan and Proteasome inhibitors bortezomib and S-2209. |
| In vivo study | Resminostat oral 600 mg once daily was well tolerated for 1-5 days in a 14 day cycle. Resminostat showed good PK profile with high bioavailability and low mutation rate. Resminostat oral apparent t 1/2 from 2.7 to 4.4 hours. Modulation of plasma biomarkers further indicates the activity of the drug. |
864814-88-0 - Preparation solution concentration reference
| 1mg | 5mg | 10mg | |
|---|---|---|---|
| 1 mM | 2.862 ml | 14.31 ml | 28.62 ml |
| 5 mM | 0.572 ml | 2.862 ml | 5.724 ml |
| 10 mM | 0.286 ml | 1.431 ml | 2.862 ml |
| 5 mM | 0.057 ml | 0.286 ml | 0.572 ml |
Last Update：2024-01-02 23:10:35
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View History
864814-88-0
105827-78-9
3-PHENOXYBENZOIC ACID HYDRAZIDE
4-METHOXYBENZYLZINC CHLORIDE
141942-85-0
Bromoethylphenylsulfide
ethyl cyclobutanecarboxylate
2BA 对乙基苯甲酸
SALOR-INT L210005-1EA
乙二胺四乙酸-D12酸
105827-78-9
3-PHENOXYBENZOIC ACID HYDRAZIDE
4-METHOXYBENZYLZINC CHLORIDE
141942-85-0
Bromoethylphenylsulfide
ethyl cyclobutanecarboxylate
2BA 对乙基苯甲酸
SALOR-INT L210005-1EA
乙二胺四乙酸-D12酸