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CCG-222740

Cat. No. M10498

All AbMole products are for research use only, cannot be used for human consumption.

CCG-222740 Structure
Size Price Availability Quantity
5mg USD 280  USD280 In stock
10mg USD 440  USD440 In stock
25mg USD 780  USD780 In stock
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Quality Control & Documentation
Biological Activity

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.

Protocol (for reference only)
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
Chemical Information
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
References

[1] Ana S Leal, et al. Sci Rep. The Rho/MRTF pathway inhibitor CCG-222740 reduces stellate cell activation and modulates immune cell populations in Kras G12D; Pdx1-Cre (KC) mice

[2] Cynthia Yu-Wai-Man, et al. Sci Rep. Local delivery of novel MRTF/SRF inhibitors prevents scar tissue formation in a preclinical model of fibrosis

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Keywords: CCG-222740 supplier, Ras, inhibitors, activators

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