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CCG-222740

Chemical Structure : CCG-222740

CAS No.: 1922098-69-8

CCG-222740 (CCG222740)

Catalog No.: PC-35330Not For Human Use, Lab Use Only.

CCG-222740 (CCG222740) is a pharmacological inhibitor of MRTF/SRF signalling, shows greater inhibitory effect on MRTF/SRF target genes than MRTF-A inhibitor CCG-203971, with IC50 of 5 uM in fibroblast-mediated collagen contraction assay.

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Purity & Documentation Purity: >98% (HPLC)

Biological Activity

CCG-222740 (CCG222740) is a pharmacological inhibitor of MRTF/SRF signalling, shows greater inhibitory effect on MRTF/SRF target genes than MRTF-A inhibitor CCG-203971, with IC50 of 5 uM in fibroblast-mediated collagen contraction assay; CCG-222740 is a more potent inhibitor of alpha-smooth muscle actin protein expression than CCG-203971; prevents scar tissue formation in a preclinical model of fibrosis; effectively kills BRAFi-resistant melanoma cells.

Physicochemical Properties

M.Wt 444.863
Formula C23H19ClF2N2O3
Appearance Solid
CAS No.
Storage
Solide Powder
-20 °C 12 Months; 4°C 6 Months
In Solvent
-80 °C 6 Months; -20°C 6 Months
Shipping
Solubility

10 mM in DMSO

Chemical Name/SMILES

N-(4-chlorophenyl)-5,5-difluoro-1-(3-(furan-2-yl)benzoyl)piperidine-3-carboxamide

References

1. Hutchings KM, et al. Bioorg Med Chem Lett. 2017 Apr 15;27(8):1744-1749.

2. Yu-Wai-Man C, et al. Sci Rep. 2017 Mar 31;7(1):518.

3. Sean A. Misek, et al. Abstract 5895: Targeting RhoA-regulated gene transcription in drug-resistant melanoma. AACR 2018.

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