UNC0638 is a potent, selective and cell-penetrant chemical probe for G9a and GLP with IC50 of <15 nM and 19 nM, respectively, shows selectivity over a wide range of epigenetic and non-epigenetic targets.
 |
Source | Oncol Lett (2015). Figure 2. UNC0638 |
| Method | transwell assay | |
| Cell Lines | MDA.MB.231 and BT.549 cells | |
| Concentrations | 0.5 and 1 μM | |
| Incubation Time | 24 h | |
| Results | UNC0638 treatment significantly decreased the ability of TNBC cells to migrate and recover the wounded area. |
| Molecular Weight | 509.73 |
| Formula | C30H47N5O2 |
| CAS Number | 1255580-76-7 |
| Solubility (25°C) | DMSO >10 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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