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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 |
| Molecular Weight | 444.86 |
| Formula | C23H19ClF2N2O3 |
| CAS Number | 1922098-69-8 |
| Form | Solid |
| Solubility (25°C) | DMSO 90 mg/mL |
| Storage |
Powder -20°C 3 years ; 4°C 2 years In solvent -80°C 6 months ; -20°C 1 month |
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