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CCG-222740 is a selective, orally active Rho/myocardin-related transcription factor (MRTF) pathway inhibitor. CCG-222740 is also a potent inhibitor of alpha-smooth muscle actin protein expression. CCG-222740 markedly decreased SRF reporter gene activity and showed a greater inhibitory effect on MRTF/SRF target genes than the previously described MRTF-A inhibitor CCG-203971. CCG-222740 increases the protein levels of p27 and decreased cyclin D1. CCG-222740 treatment decreased cell viability of CAFs, with an IC50 of~10 μM.
In vivo, CCG-222740 (100 mg/kg; oral gavage for 7 days) significantly reduces α-SMA levels in the pancreas of caerulein-stimulated KC mice.
| Cell Experiment | |
|---|---|
| Cell lines | Cancer associated fibroblasts (CAFs) |
| Preparation method | Murine cancer associated fibroblasts (CAFs) are cultured in DMEM supplemented with 10% fetal bovine serum(FBS). CAFs are treated with several concentrations of CCG-222740 (740) for 72 hours, and levels of Cyclin D1 and p27 are evaluated by western blot. |
| Concentrations | 10 μM |
| Incubation time | 72 h |
| Animal Experiment | |
|---|---|
| Animal models | Nine-week old KC mice |
| Formulation | dissolved in 15% (v/v) DMSO and then added to a solution of 10% tween-20 in saline |
| Dosages | 100 mg/kg |
| Administration | Oral gavage; daily; for 7 days |
| 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.
| Molecular Weight | 444.86 |
| Formula | C23H19ClF2N2O3 |
| CAS Number | 1922098-69-8 |
| Purity | >99% |
| Solubility | DMSO 90 mg/mL |
| Storage | at -20°C |
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