CUDC-101 is a potent multitargeted HDAC, EGFR and HER2 inhibitor with IC50 of 4.4, 2.4, and 15.7 nM, respectively. CUDC-101 synergistically blocked key regulators of EGFR/HER2 signaling pathways, also attenuating multiple compensatory pathways, such as AKT, HER3, and MET, which enable cancer cells to escape the effects of conventional EGFR/HER2 inhibitors.
 |
Source | Oncotarget (2015). Figure 5. CUDC-101 |
| Method | Apoptosis arrays | |
| Cell Lines | ATC cells | |
| Concentrations | 1.1 μM | |
| Incubation Time | 24 h | |
| Results | Treatment with CUDC-101 also significantly reduced the expression of survivin and XIAP, known inhibitors of caspases |
| Cell Experiment | |
|---|---|
| Cell lines | A431, H292 and BT474 cells |
| Preparation method | Cell growth, viability, and apoptosis assay Cancer cell lines were obtained from the American Type Culture Collection and were maintained according to the supplier's instructions. Cancer cell lines were plated at 5,000 to 10,000 cells per well in 96-well flat-bottomed plates with varying concentrations of compounds. The cells were incubated with compounds for 72 hours in the presence of 0.5% of fetal bovine serum. Growth inhibition was assessed by an ATP content assay using the Perkin-Elmer ATPlite kit. Apoptosis was routinely assessed by measuring the activities of caspase-3 and caspase-7 using the Promega Apo-ONE Homogeneous Assay kit. |
| Concentrations | 0, 0.1, 1, or 10 µM |
| Incubation time | 72h |
| Animal Experiment | |
|---|---|
| Animal models | HepG2 hepatoma cells xenograft models nude mice |
| Formulation | 30% Captisol solution |
| Dosages | 120 mg/kg daily |
| Administration | i.v./i.p |
| Molecular Weight | 434.49 |
| Formula | C24H26N4O4 |
| CAS Number | 1012054-59-9 |
| Solubility (25°C) | DMSO 20 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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