Vorinostat (SAHA, Zolinza, MK-0683) is a selective and potent histone deacetylase (HDAC) inhibitor with the IC50 value of 10 nM for HDAC-1.The pan-HDAC inhibitor vorinostat (SAHA,Zolinza,MK-0683) potentiates the activity of the proteasome inhibitor carfilzomib in human DLBCL cells in vitro and in vivo.Vorinostat (SAHA, Zolinza, MK-0683),which also inhibits HDAC6,could enhance the activity of the novel proteasome inhibitor CFZ in DLBCL cells, including those resistant to bortezomib alone.
BMC Cancer. 2016 Nov 7;16(1):857.
Vorinostat enhances the cisplatin-mediated anticancer effects in small cell lung cancer cells.
Vorinostat purchased from AbMole
Cell Experiment | |
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Cell lines | HH, HuT78, MJ, MylA and SeAx cells |
Preparation method | cell viability assay. The inhibitory effect of vorinostat on the viability of CTCL cell lines was examined through a CellTiter-Glo assay using various concentrations of vorinostat (0.01, 0.05, 0.15, 0.5, 1.25, 4, 10, 35, and 100 μM) for 72 h. All CTCL cell lines were sensitive to the investigated HDAC inhibitor. The inhibitory effect of vorinostat was reflected as a dose-dependent reduction in cell proliferation/viability. The IC50 of proliferation was determined at 0.146 μM in HH cells, at 2.062 μM in HuT78 cells, at 2.697 μM in MJ cells, at 1.375 μM in MylA and at 1.510 μM in SeAx cells. |
Concentrations | 0.01, 0.05, 0.15, 0.5, 1.25, 4, 10, 35, and 100 μM |
Incubation time | 72 h |
Animal Experiment | |
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Animal models | R6/2 mice motor impair |
Formulation | solubilized in 5 molar equivalents of HOP-β-CD (ICN) in water |
Dosages | 0.67g/L |
Administration | orally |
Molecular Weight | 264.3 |
Formula | C14H20N2O3 |
CAS Number | 149647-78-9 |
Solubility (25°C) | DMSO 55 mg/mL |
Storage |
Powder -20°C 3 years ; 4°C 2 years In solvent -80°C 6 months ; -20°C 1 month |
Species | Mouse | Rat | Rabbit | Guinea pig | Hamster | Dog |
Weight (kg) | 0.02 | 0.15 | 1.8 | 0.4 | 0.08 | 10 |
Body Surface Area (m2) | 0.007 | 0.025 | 0.15 | 0.05 | 0.02 | 0.5 |
Km factor | 3 | 6 | 12 | 8 | 5 | 20 |
Animal A (mg/kg) = Animal B (mg/kg) multiplied by | Animal B Km |
Animal A Km |
For example, to modify the dose of Compound A used for a mouse (20 mg/kg) to a dose based on the BSA for a rat, multiply 20 mg/kg by the Km factor for a mouse and then divide by the Km factor for a rat. This calculation results in a rat equivalent dose for Compound A of 10 mg/kg.
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