Belinostat (PXD101) is a novel HDAC inhibitor with an IC50 of 27 nM. Belinostat (PXD101) is cytotoxic in vitro in a number of tumor cell lines with IC50s in the range 0.2-3.4 µM as determined by a clonogenic assay and induces apoptosis. This hdac inhibitor is currently under phase I/II testing in lymphoma, ovarian cancer and other solid tumors.
| Cell Experiment | |
|---|---|
| Cell lines | A2780, A2780/cp70, CALU-3, MCF7, PC3, HS852, HT29 and HCT116 cell lines |
| Preparation method | Cytotoxicity Assay. Drug sensitivity was determined by a clonogenic assay (13). Briefly, cells were plated in 5 ml of medium at a density of 8 × 104 cells/25 cm2 flask and allowed to attach and grow for 48 h. Cells were exposed to drug (five concentrations from 0.016 to 10 μM) for 24 h. The medium was removed, and 1 ml of trypsin/EDTA was added to each flask. Once the cells had detached, 1 ml of medium was added, the cells were resuspended, and those from the control untreated flask were counted. Cells were diluted and plated into 6-cm Petri dishes (three per flask) at a density of 500-2000 cells/dish depending on the cell line. Cells from the drug-treated flasks were diluted and plated as for the control flasks. Dishes were incubated for 10–15 days at 37°C. Cells were washed with PBS, fixed in methanol, and stained with crystal violet, and colonies that contained ≥50 cells counted. Sensitivity is expressed as the IC50 (mean ± SE of three experiments) defined as the concentration of drug required to reduce the number of colonies to 50% of that of the control untreated cells. |
| Concentrations | 0.016 ~ 10 μM |
| Incubation time | 24 h |
| Animal Experiment | |
|---|---|
| Animal models | A2780, A2780/cp70 and HCT116 tumor-bearing mice model |
| Formulation | dissolved in DMSO and then diluted in water to give a final concentration of DMSO of 10% |
| Dosages | a single injection of 40 mg/kg |
| Administration | i.p. |
| Molecular Weight | 318.35 |
| Formula | C15H14N2O4S |
| CAS Number | 414864-00-9 |
| Solubility (25°C) | DMSO 60 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.
| Related HDAC Products |
|---|
| Ac-Arg-Gly-Lys(Ac)-AMC
Ac-Arg-Gly-Lys(Ac)-AMC is a substrate for HDAC. |
| Chlamydocin
Chlamydocin, a fungal metabolite, is a highly potent HDAC inhibitor, with an IC50 of 1.3 nM. |
| HDAC-IN-30
HDAC-IN-30 is a novel multi-target HDAC inhibitor, including HDAC1 (IC50=13.4 nM),HDAC2 (IC50=28.0 nM), HDAC3 (IC50=9.18 nM), HDAC6 (IC50=42.7 nM), HDAC8 (IC50=131 nM). |
| Ac-Arg-Gly-Lys(Ac)-AMC acetate
Ac-Arg-Gly-Lys(Ac)-AMC acetate is a substrate for histone deacetylase (HDAC) and can be used in a novel fluorescent assay for HDAC activity. |
| JPS014 TFA
JPS014 TFA is a benzamide-based Von Hippel-Lindau (VHL) E3-ligase proteolysis targeting chimeras (PROTAC). |
Products are for research use only. Not for human use. We do not sell to patients.
© Copyright 2010-2023 AbMole BioScience. All Rights Reserved.
