CCG-222740 is an orally active and selective Rho/myocardin-related transcription factor (MRTF) pathway inhibitor. CCG-222740 is also a potent inhibitor of alpha-smooth muscle actin protein expression. CCG-222740 effectively reduces fibrosis in skin and blocks melanoma metastasis.
IC50&Target
Rho/MRTF pathway
体外研究
CCG-222740 (10, 20 μM; for 72 hours) increases the protein levels of p27 and decreases cyclin D1. CCG-222740 decreases cell viability of CAFs, with an IC50 of ~10 μM.
CCG-222740 (10, 25 μM) is potent at decreasing αSMA protein expression in human conjunctival fibroblasts.
CCG-222740 has an IC50 of 5 μM in a fibroblast-mediated collagen contraction assay, and it is less cytotoxic.
Cell Cycle Analysis
Cell Line:
Cancer associated fibroblasts (CAFs)
Concentration:
10, 20 μM
Incubation Time:
72 hours
Result:
Increased the protein levels of p27 and decreased cyclin D1.
体内研究
CCG-222740 (oral gavage; 100 mg/kg/day for 7 days) significantly reduces α-SMA levels in the pancreas of caerulein-stimulated KC mice.
Animal Model:
KC mice (LSL-Kras; Pdx-1-Cre) of age at 9 weeks
Dosage:
100 mg/kg
Administration:
Oral gavage; daily; for 7 days
Result:
Reduced α-SMA levels in the pancreas of caerulein-stimulated KC mice.
分子式
C23H19ClF2N2O3
分子量
444.86
CAS号
1922098-69-8
运输条件
Room temperature in continental US; may vary elsewhere.