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CCG-222740

Cat. No. M10498
CCG-222740 Structure
Size Price Availability Quantity
5mg USD 345  USD345 In stock
10mg USD 540  USD540 In stock
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Quality Control
  • Current batch:
  • Purity >99%
  • COA
  • MSDS
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
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
Conversion of different model animals based on BSA (Value based on data from FDA Draft Guidelines)
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.

Chemical Information
Molecular Weight 444.86
Formula C23H19ClF2N2O3
CAS Number 1922098-69-8
Purity >99%
Solubility DMSO 90 mg/mL
Storage at -20°C
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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