For research use only. Not for therapeutic Use.
CCG-203971 is an inhibitor of SRE activation in the prostate cancer cell line PC-3 (IC50 = 6.4 μM), with 87% inhibition of SRE activation achieved at 100 μM. This compound also inhibits PC-3 cell migration (IC50 = 4.2 μM), as determined by a scratch wound assay
| Catalog Number | R014451 |
| CAS Number | 1443437-74-8 |
| Synonyms | N-(4-Chlorophenyl)-1-[3-(2-furanyl)benzoyl]-3-piperidinecarboxamide; |
| Molecular Formula | C23H21ClN2O3 |
| Purity | ≥95% |
| Target | Transcription Factors |
| Solubility | Soluble in DMSO > 10 mM |
| Storage | Store at +4°C |
| IUPAC Name | N-(4-chlorophenyl)-1-[3-(furan-2-yl)benzoyl]piperidine-3-carboxamide |
| InChI | InChI=1S/C23H21ClN2O3/c24-19-8-10-20(11-9-19)25-22(27)18-6-2-12-26(15-18)23(28)17-5-1-4-16(14-17)21-7-3-13-29-21/h1,3-5,7-11,13-14,18H,2,6,12,15H2,(H,25,27) |
| InChIKey | HERLZBNILRVHQN-UHFFFAOYSA-N |
| SMILES | C1CC(CN(C1)C(=O)C2=CC=CC(=C2)C3=CC=CO3)C(=O)NC4=CC=C(C=C4)Cl |
| Reference | 1:Bioorg Med Chem Lett. 2017 Apr 15;27(8):1744-1749. doi: 10.1016/j.bmcl.2017.02.070. Epub 2017 Mar 10. Pharmacokinetic optimitzation of CCG-203971: Novel inhibitors of the Rho/MRTF/SRF transcriptional pathway as potential antifibrotic therapeutics for systemic scleroderma.Hutchings KM,Lisabeth EM,Rajeswaran W,Wilson MW,Sorenson RJ,Campbell PL,Ruth JH,Amin A,Tsou PS,Leipprandt JR,Olson SR,Wen B,Zhao T,Sun D,Khanna D,Fox DA,Neubig RR,Larsen SD, PMID: 28285914 PMCID: PMC5395305 [Available on 2018-04-15] DOI: 10.1016/j.bmcl.2017.02.070 </br><span>Abstract:</span> We recently reported the development of a novel inhibitor of Rho-mediated gene transcription (1, CCG-203971) that is efficacious in multiple animal models of acute fibrosis, including scleroderma, when given intraperitoneally. The modest in vivo potency and poor pharmacokinetics (PK) of this lead, however, make it unsuitable for long term efficacy studies. We therefore undertook a systematic medicinal chemistry effort to improve both the metabolic stability and the solubility of 1, resulting in the identification of two analogs achieving over 10-fold increases in plasma exposures in mice. We subsequently showed that one of these analogs (8f, CCG-232601) could inhibit the development of bleomycin-induced dermal fibrosis in mice when administered orally at 50mg/kg, an effect that was comparable to what we had observed earlier with 1 at a 4-fold higher IP dose.Copyright © 2017 Elsevier Ltd. All rights reserved. |
